Afshin Zarghi

[ 1 ] - Design, Synthesis and Biological Evaluation of Novel Peptide-Like Analogues as Selective COX-2 Inhibitors

A new series of peptide-like derivatives containing different aromatic amino acids andpossessing pharmacophores of COX-2 inhibitors as SO2Me or N3 attached to the para positionof an end phenyl ring was synthesized for evaluation as selective cyclooxygenase-2 (COX-2)inhibitors. The synthetic reactions were based on the solid phase peptide synthesis methodusing Wang resin. One of the analogues, i...

[ 2 ] - Physicochemical, Stress Degradation Evaluation and Pharmacokinetic Study of AZGH101; a New Synthesized COX2 Inhibitor after I.V. and Oral Administration in Male and Female Rats

Nonsteroidal anti-inflammatory drugs (NSAIDs) act mainly via inhibition of prostaglandins synthesis by inhibition of cyclooxygenase (COX) isoenzymes (COX1 and COX 2). Selective COX-2 inhibitors which are also known as coxibs provide the main therapeutic effects of NSAIDs. Zarghi et al. reported 6-benzoyl-2-(4-(methylsulfonyl)phenyl)quinoline-4-carboxylic acid (AZGH 101) as a novel derivative of...

[ 3 ] - Physicochemical, stress degradation evaluation and pharmacokinetic study of AZGH102, a new synthesized COX2 inhibitors after I.V. and oral administration in male and female rats

Coxibs such as celecoxib, rofecoxib and valdecoxib are introduced as selective COX-2 inhibitors to the market. It has been reported that inhibition of COX-2 beside traditional effects of NSAIDs, reduces the risk of colorectal, breast and lung cancers and slow the progress of Alzheimer’s disease. Zarghi et al. reported 8-benzoyl-2-(4-(methylsulfonyl)phenyl)quinoline-4-carboxylic acid (AZGH 102) ...

[ 4 ] - QSAR Modeling of COX-2 Inhibitory Activity of Some Dihydropyridine and Hydroquinoline Derivatives Using Multiple Linear Regression (MLR) Method

COX-2 inhibitory activities of some 1,4-dihydropyridine and 5-oxo-1,4,5,6,7,8-hexahydroquinoline derivatives were modeled by quantitative structure–activity relationship (QSAR) using stepwise-multiple linear regression (SW-MLR) method. The built model was robust and predictive with correlation coefficient (R2) of 0.972 and 0.531 for training and test groups, respectively. The quality of the mod...

[ 5 ] - A Simple and Specific Stability- Indicating RP-HPLC Method for Routine Assay of Adefovir Dipivoxil in Bulk and Tablet Dosage Form

A simple and reliable stability-indicating RP-HPLC method was developed and validated for analysis of adefovir dipivoxil (ADV).The chromatographic separation was performed on a C18 column using a mixture of acetonitrile-citrate buffer (10 mM at pH 5.2) 36:64 (%v/v) as mobile phase, at a flow rate of 1.5 ml/min. Detection was carried out at 260 nm and a sharp peak was obtained for ADV at a reten...

[ 6 ] - Progress in HIV-1 integrase inhibitors: A review of their chemical structure diversity

HIV-1 integrase (IN) enzyme, one of the three main enzymes of HIV-1, catalyzed the insertion of the viral DNA into the genome of host cells. Because of the lack of its homologue in human cells and its essential role in HIV-1 replication, IN inhibition represents an attractive therapeutic target for HIV-1 treatment. Since identification of IN as a promising therapeutic target, a major progress h...

[ 7 ] - Design and Synthesis of Pyrrolo[2,1-a]Isoquinoline-Based Derivatives as New Cytotoxic Agents

A new series of anti-cancer agents based on 1,2-diaryl-5,6-dihydropyrrolo[2,1-a]isoquinoline scaffold containing N,N-diethylamino‌ethoxy, piperidinyl‌ethoxy or morpholinyl‌ethoxy group at the para position of the C-2 phenyl ring were synthesized and their cytotoxic activities were assessed against several human cancer cell lines including MCF-7 (ER positive breast cancer cell), MDA-MB231 (ER-ne...

[ 8 ] - QSAR Analysis for Some 1, 2-Benzisothiazol-3-one Derivatives as Caspase-3 Inhibitors by Stepwise MLR Method

Caspase-3, one of the dominant effectors caspases, is activated in almost every model of apoptosis with various signaling pathways. Hence, inhibition of caspase-3 has become an attractive target in the treatment of neurodegenerative diseases. Caspase-3 inhibitory activities of some 1,2-benzisothiazol-3-one derivatives were modeled by quantitative structure–activity relationship (QSAR) using ste...

[ 9 ] - Design, Synthesis and Biological Evaluation of4-(Imidazolylmethyl)-2-(4-methylsulfonyl phenyl)-Quinoline Derivatives as Selective COX-2 Inhibitors and In-vitro Anti-breast Cancer Agents

A new group of 4-(Imidazolylmethyl) quinoline derivatives possessing a methylsulfonyl COX-2 pharmacophore at the para position of the C-2 phenyl ring were designed and synthesized as selective COX-2 inhibitors and in-vitro anti breast cancer agents. In-vitro COX-1 and COX-2 inhibition studies showed that all the compounds were potent and selective inhibitors of the COX-2 isozyme with IC50 value...

[ 10 ] - Development and Validation of an HPLC Method for Determination of Amifostine and/or Its Metabolite (WR-1065) In Human Plasma Using OPA Derivatization and UV Detection

A rapid, sensitive and reproducible HPLC method was developed and validatedfor the analysis of amifostine (AMF) and/or its metabolite, WR-1065 inhuman plasma. The method involves the alkylation of free sulfydryl group with iodoacetic acid followed by derivatization of the drug and its metabolite witho-phthaldialdehyde (OPA) andUVdetection at 340 nm. The derivatized AMF and WR-1065 were eluted i...

[ 11 ] - Design, Synthesis and Biological Evaluation of new 1,4-Dihydropyridine (DHP) Derivatives as Selective Cyclooxygenase-2 Inhibitors

As a continuous research for discovery of new COX-2 inhibitors, chemical synthesis, in vitro biological activity and molecular docking study of anew group of 1,4-dihydropyridine (DHP) derivatives were presented. Novel synthesized compounds possessing a COX-2 SO2Me pharmacophore at the para position of C-4 phenyl ring, different hydrophobic groups (R1) at C-2 position and alkoxycarbonyl groups (...

[ 12 ] - QSAR Study on Anti-HIV-1 Activity of 4-Oxo-1,4-dihydroquinoline and 4-Oxo-4H-pyrido[1,2-a]pyrimidine Derivatives Using SW-MLR, Artificial Neural Network and Filtering Methods

Predictive quantitative structure–activity relationship was performed on the novel 4-oxo-1,4-dihydroquinoline and 4-oxo-4H-pyrido[1,2-a]pyrimidine derivatives to explore relationship between the structure of synthesized compounds and their anti-HIV-1 activities. In this way, the suitable set of the molecular descriptors was calculated and the important descriptors using the variable selections ...

[ 13 ] - Design, Synthesis and Cytotoxicity Evaluationof New 1,2-diaryl-4, 5, 6, 7-Tetrahydro-1H-benzo[d] Imidazolesas Tubulin Inhibitors

A new series of 1,2-diaryl-4,5,6,7-tetrahydro-1H-benzo[d]imidazoles, possessing trimethoxy phenyl pharmacophore, were synthesized to evaluate their biological activities as tubulin inhibitors. Cytotoxic activity of the synthesized compounds 7a-f was assessed against several human cancer cell lines, including MCF-7 (breast cancer cell), HEPG2 (liver hepatocellular cells), A549 (adenocarcinomic h...

[ 14 ] - In-silico Investigation of Tubulin Binding Modes of a Series of Novel Antiproliferative Spiroisoxazoline Compounds Using Docking Studies

Interference with microtubule polymerization results in cell cycle arrest leading to cell death. Colchicine is a well-known microtubule polymerization inhibitor which does so by binding to a specific site on tubulin. A set of 3',4'-bis (substituted phenyl)-4'H-spiro[indene-2,5'-isoxazol]-1(3H)-one derivatives with known antiproliferative activities were evaluated for their tubulin binding modes...

[ 15 ] - Search for the Pharmacophore of Histone Deacetylase Inhibitors Using Pharmacophore Query and Docking Study

Histone deacetylase inhibitors have gained a great deal of attention recently for the treatment of cancers and inflammatory diseases. So design of new inhibitors is of great importance in pharmaceutical industries and labs. Creating pharmacophor models in order to design new molecules or search a library for finding lead compounds is of great interest. This approach reduces the overall cost ass...

[ 16 ] - Cytotoxicity of Selected Novel Chalcone Derivatives on Human Breast, Lung and Hepatic Carcinoma Cell Lines

Cancer is considered as a challenging deathly disease and discovering or synthesis of new cytotoxic agents is a worldwide attempt. In this study, a group of recently synthesized chalcones, with the structure of 1,3-diarylprop-2-en-1-one having differesnt COX-1 and/or COX-2 selectivities, have been examined on human hepatocarcinoma (HepG2), lung carcinoma (A549), and breast adenocarcinoma (MCF-7...

[ 17 ] - Design, Synthesis and Biological Evaluation of 5-Oxo-1,4,5,6,7,8 Hexahydroquinoline Derivatives as Selective Cyclooxygenase-2 Inhibitors

A group of regioisomeric 5-oxo-1,4,5,6,7,8 hexahydroquinoline derivatives possessing a COX-2 SO2Me pharmacophore at the para position of the C-2 or C-4 phenyl ring, in conjunction with a C-4 or C-2 phenyl (4-H) or substituted-phenyl ring (4-F,4-Cl,4-Br,4-OMe,4-Me, 4-NO2), were designed for evaluation as selective cyclooxygenase-2 (COX-2) inhibitors. These target 5-oxo-1,4,5,6,7,8 hexahydroquino...

[ 18 ] - Design, Synthesis and Cytotoxicity Evaluation of New 2-Aryl-5,6-Dihydropyrrolo[2, 1-a]Isoquinoline Derivatives as Topoisomerase Inhibitors

Two set of 2-aryl-5,6-dihydropyrrolo[2,1-a] isoquinolines were designed and synthesized to evaluate their biological activities as topoisomerase inhibitors. Cytotoxic activity of the synthesized compounds 4a-e and 7a-d was assessed against several human cancer cell lines, including MCF-7 (breast cancer cell), HepG2 (liver hepatocellular cells), A549 (adenocarcinomic human alveolar basal epithel...

[ 19 ] - Occurrence of Deoxynivalenol in Foods for Human Consumption from Tehran, Iran

AbstractThe occurrence of deoxynivalenol (DON) in retail foods in Tehran (Iran) was determined using high-performance liquid chromatography technique and immunoaffinity column as the clean-up step. A method was validated for analysis of DON in rice, bread, puffed corn snack and wheat flour. The average recoveries and precision (RSD) for DON in different foods ranged 84.2-93.1% and 2.9-12.0%, re...

[ 20 ] - Rapid High Performance Liquid Chromatographic Method for Determination of Clarithromycin in Human Plasma Using Amperometric Detection: Application in Pharmacokinetic and Bioequivalence Studies

A rapid, sensitive and reproducible HPLC method using amperometric detector was developed and validated for the analysis of clarithromycin in human plasma. The separation was achieved on a monolithic silica column (MZ- C8 125×4.0 mm) using acetonitrile- methanol-potassium dihydrogen phosphate buffer (40:6:54,v/v), with pH of 7.5, as the mobile phase at a flow rate of 1.5 mL/min. The assay enabl...

[ 21 ] - Improvement of Capillary Electrophoretic Enantioseparation of Fluoxetine by a Cationic Additive

One of the problems encountered in CE separations of basic compounds is the adsorption of analytes onto the negatively charged capillary wall which could lead to poor repeatability of migration time and peak area. Additionally, separation of enantiomers of chiral of basic drugs is commonly carried out in low pH buffer which contributes to strong ionic interaction of the cationic drug ions with ...

[ 22 ] - Analysis of Aflatoxin B1 in Iranian Foods Using HPLC and a Monolithic Column and Estimation of its Dietary Intake

A high performance liquid chromatographic method was developed for determination of aflatoxin B1 (AFB1) in foods using a monolithic column with sample clean up on an immunoaffinity column. The method was validated for analysis of AFB1 in rice, bread, puffed corn snack, wheat flour and peanut samples. The average recoveries for AFB1 in different foods ranged from 94.4 to 102.5% with the coeffici...

[ 23 ] - Evaluation of Anti-nociceptive and Anti-inflammatory Activities of Novel Chalcone Derivatives

Chalcone (1,3-diarylprop-2-en-1-one) derivatives have been introduced as selective cyclooxygenase-2 inhibitors. In the present study, anti-nociceptive and anti-inflammatory effects of eight novel compounds were evaluated in male mice and Wistar rats by using the writhing and formalin-induced paw edema tests respectively. The activities of the compounds were compared with celecoxib as a referenc...

[ 24 ] - Physical and Chemical Stability of Mycophenolate Mofetil (MMF) Suspension Prepared at the Hospital

To evaluate the physical and chemical stability of a suspension of mycophenolate mofetil (MMF) prepared in the hospital from commercially available MMF capsules and tablets. Extemporaneous pharmacy was used as a feasible method in this experimental study to prepare suspension form of MMF. Suspension formulations were prepared from both tablets and capsules forms of MMF. Thereafter the stability...

[ 25 ] - Exposure Assessment of the Tehran Population (Iran) to Zearalenone Mycotoxin

Zearalenone (ZEA) mycotoxin is a potent estrogenic metabolite. It is the primary toxin causing infertility, abortion or other breeding problems. A HPLC method was validated for ZEA in foods using a monolithic column with sample clean-up on an immunoaffinity column. A certified reference material (CRM) from FAPAS (UK) was analyzed. A survey of ZEA was performed on the 72 samples of rice, bread, ...

[ 26 ] - Selective COX-2 Inhibitors: A Review of Their Structure-Activity Relationships

Non-steroidal anti-inflammatory drugs (NSAIDs) are the competitive inhibitors of cyclooxygenase (COX), the enzyme which mediates the bioconversion of arachidonic acid to inflammatory prostaglandins (PGs). Their use is associated with the side effects such as gastrointestinal and renal toxicity. The therapeutic anti-inflammatory action of NSAIDs is produced by the inhibition of COX-2, while the ...

[ 27 ] - Synthesis and Cytotoxic Evaluation of Some Novel Sulfonamide Derivatives Against a Few Human Cancer Cells

Sulfonamides are the first effective chemotherapeutic agents used for several years to cure or prevent systemic bacterial infections. In addition, this agents showed anti-carbonic anhydrase and cause cell cycle perturbation in the G1 phase, disruption of microtubule assembly, suppression of the transcription activator Nf-Y, angiogenesis and matrix metalloproteinase (MMP). In recent years, novel...

[ 28 ] - Quantification of Polyethylene Glycol Esters of Methotrexate and Determination of Their Partition Coefficients by Validated HPLC Methods

Conjugation of methotrexate (MTX) (MW 454) with different molecular weights of polyethylene glycol (PEG) including methoxy-peg (mpeg) 750 D and 5000 D and diol-peg 35000 D led to compounds that are physicochemically highly different from the parent compound, MTX. In this study, an HPLC system consisting of C8 column and UV detector (?=342 nm), using a mixture of 30:70 v/v phosphate-citrate buff...

[ 29 ] - The Pharmacological Effects of Odonthobuthus doriae Scorpion Venom and Its Extracted Fractions on Neuro-Muscular Transmission

The effect of Odonthobuthos doriae (O.d) scorpion venom at 0/3, 1 and 3, 10 µg/ml concentrations were investigated on nerve-muscle transmission, using the Twitch tension technique. A concentration of 0.3 µg/ml caused a small change in the twitch height in response to indirect muscle stimulation, but higher concentrations (1, 3, 10 µg/ml) caused a transient augmentation in twitch response follow...

[ 30 ] - Rapid High Performance Liquid Chromatographic Determination of Risperidone in Human Plasma

A simple, rapid and sensitive high-performance liquid chromatographic (HPLC) method for the determination of risperidone in human plasma was developed. An HPLC system based on a Nucleosil C8 column (150?4 mm) and a UV detector (?= 280 nm) were used. A mixture of sodium dihydrogen phosphate buffer-acetonitrile (55:45, v/v) adjusted to pH 6.0 at a flow rate of 1.5 ml min-1 was used as mobile phas...

[ 31 ] - Survey of fumonisin B1 contamination of cornin Northern Iran during 2000

Fumonisin B1 (FB1) is the most abundant of the fumonisin mycotoxins, mainly produced in corn by fungi of the genus Fusarium. FB1 has been shown to be hepatocarcinogenic and nephrocarcinogenic in animals. Contamination of corn with FB1 was assayed in samples collected from Mazandaran Province, situated on the Caspian littoral of Iran, in September 2000. In this survey, 38 corn samples were analy...

[ 32 ] - Design and Synthesis of New Imidazole Derivatives of Captopril

A new series of alkylthio imidazole analogues of captopril, an ACE inhibitor used in the treatment of hypertension, was designed and synthesized in order to obtain agents more active than captopril with less side effects. All the compounds thus prepared were purified and characterized by IR, NMR and Mass analytical instruments.

[ 33 ] - Enhancement of percutaneous absorption of curcumin (turmeric pigment) by ethanol

Curcumin is the active component of Curcuma species including C. longa (turmeric). This molecule is well known for its anti-inflammatory effect, which seems to be stronger than that of hydrocortisone. Curcuma species have been used in Asian traditional medicine as topical anti-inflammatory drugs. Curcumin has poor oral bioavailability and its topical application could be of choice, particularly...

[ 34 ] - Separation of Somatropin and Its Degradation Products by High-Performance Liquid Chromatography Using a Reversed-Phase Polymeric Column

The accurate prediction of protein stability is one of the most challenging goals in protein formulation and delivery. In this study, a gradient RP-HPLC method is described for the separation of human growth hormone (hGH) variants as deamidated and oxidized forms. The methodology employed a polymeric poly (styrene-co-divinylbenzene) column and a 1mL/min flow rate of a linear gradient of 0.1% v/...

[ 35 ] - Stereoselective Permeation of Tretinoin and Isotretinoin through Enhancer-Treated Rat Skin. II. Effects of Lipophilic Penetration Enhnacers

Many properties of chemicals depend on their stereochemistry. Among these, the effects of stereoisomerism on percutaneous absorption of drugs are not well studied. We have previously shown that permeation of tretinoin and isotretinoin (two geometric isomers) through hydrophilic enhancers-treated rat skin is stereoselective. As, depending on their lipophilicity, penetration enhancers can change ...

[ 36 ] - Stereoselective Permeation of Tretinoin and Isotretinoin through Enhancer-Treated Rat Skin. I. Effect of Ethanol and Sodium Dodecyl Sulfate

Many properties of chemicals depend on their streochemistry. Among these, the effects of streoisomerism on percutaneous absorption of drugs, which is subject of the present investigation, is not well studied yet. In this study, tretinoin (TT) and isotretinoin (ITT) (geometric isomers) were chosen and their permeations (alone or in the presence of each other) through enhancer-treated excised ...

[ 37 ] - Bioequivalence Studies of Two Formulations of Baclofen Tablet in Healthy Volunteers

The relative bioavailability of the test (generic) product 2 × 25 mg baclofen tablets, with respect to the reference product, Lioresal® 2 × 25 mg tablets (baclofen; Squibb) was determined in a single-blind, single dose, randomised, crossover study. The mean values for the variable Cmax were 737.6 ng/ml for the reference and 739.5 ng/ml for the test product. The mean values for the variable AUC ...

[ 38 ] - A Modified Method for the Synthesis of Nitrofurazone

Nitrofurazone is one of the antibacterial nitrofuran agents used topically for skin infections. The drug is effective on the majority of infectious microorganisms. Because of the importance of this drug in clinic, in this study various methods of synthesis of nitrofurazone were examined and the most appropriate method, applicable to pharmaceutical industry was chosen and optimized from the poin...

[ 39 ] - Synthesis and Biological Evaluation of New 1, 4-Dihydropyridines as Antihypertensives Agents in Rats

New analogues of nifedipine, as a known calcium channel blocker, were synthesized by replacing the orthonitrophenyl group on position 4 with 1-(4-Nitrobenzyl)-5-imidazolyl or 2-methylthio-1-(4-Nitrobenzyl)-5-imidazolyl substituent. Effects of the new synthesized compounds on blood pressure were studied at 15, 30 and 60 min after administration by indirect tail-cuff method and compared with nife...

[ 40 ] - Design, Synthesis and Biological Evaluation of Novel Peptide-Like Analogues as Selective COX-2 Inhibitors

A new series of peptide-like derivatives containing different aromatic amino acids andpossessing pharmacophores of COX-2 inhibitors as SO2Me or N3 attached to the para positionof an end phenyl ring was synthesized for evaluation as selective cyclooxygenase-2 (COX-2)inhibitors. The synthetic reactions were based on the solid phase peptide synthesis methodusing Wang resin. One of the analogues, i...

[ 41 ] - Physicochemical, Stress Degradation Evaluation and Pharmacokinetic Study of AZGH101; a New Synthesized COX2 Inhibitor after I.V. and Oral Administration in Male and Female Rats

Nonsteroidal anti-inflammatory drugs (NSAIDs) act mainly via inhibition of prostaglandins synthesis by inhibition of cyclooxygenase (COX) isoenzymes (COX1 and COX 2). Selective COX-2 inhibitors which are also known as coxibs provide the main therapeutic effects of NSAIDs. Zarghi et al. reported 6-benzoyl-2-(4-(methylsulfonyl)phenyl)quinoline-4-carboxylic acid (AZGH 101) as a novel derivative of...

[ 42 ] - Physicochemical, stress degradation evaluation and pharmacokinetic study of AZGH102, a new synthesized COX2 inhibitors after I.V. and oral administration in male and female rats

Coxibs such as celecoxib, rofecoxib and valdecoxib are introduced as selective COX-2 inhibitors to the market. It has been reported that inhibition of COX-2 beside traditional effects of NSAIDs, reduces the risk of colorectal, breast and lung cancers and slow the progress of Alzheimer’s disease. Zarghi et al. reported 8-benzoyl-2-(4-(methylsulfonyl)phenyl)quinoline-4-carboxylic acid (AZGH 102) ...

[ 43 ] - QSAR Modeling of COX-2 Inhibitory Activity of Some Dihydropyridine and Hydroquinoline Derivatives Using Multiple Linear Regression (MLR) Method

COX-2 inhibitory activities of some 1,4-dihydropyridine and 5-oxo-1,4,5,6,7,8-hexahydroquinoline derivatives were modeled by quantitative structure–activity relationship (QSAR) using stepwise-multiple linear regression (SW-MLR) method. The built model was robust and predictive with correlation coefficient (R2) of 0.972 and 0.531 for training and test groups, respectively. The quality of the mod...

[ 44 ] - A Simple and Specific Stability- Indicating RP-HPLC Method for Routine Assay of Adefovir Dipivoxil in Bulk and Tablet Dosage Form

A simple and reliable stability-indicating RP-HPLC method was developed and validated for analysis of adefovir dipivoxil (ADV).The chromatographic separation was performed on a C18 column using a mixture of acetonitrile-citrate buffer (10 mM at pH 5.2) 36:64 (%v/v) as mobile phase, at a flow rate of 1.5 ml/min. Detection was carried out at 260 nm and a sharp peak was obtained for ADV at a reten...

[ 45 ] - Progress in HIV-1 integrase inhibitors: A review of their chemical structure diversity

HIV-1 integrase (IN) enzyme, one of the three main enzymes of HIV-1, catalyzed the insertion of the viral DNA into the genome of host cells. Because of the lack of its homologue in human cells and its essential role in HIV-1 replication, IN inhibition represents an attractive therapeutic target for HIV-1 treatment. Since identification of IN as a promising therapeutic target, a major progress h...

[ 46 ] - Design and Synthesis of Pyrrolo[2,1-a]Isoquinoline-Based Derivatives as New Cytotoxic Agents

A new series of anti-cancer agents based on 1,2-diaryl-5,6-dihydropyrrolo[2,1-a]isoquinoline scaffold containing N,N-diethylamino‌ethoxy, piperidinyl‌ethoxy or morpholinyl‌ethoxy group at the para position of the C-2 phenyl ring were synthesized and their cytotoxic activities were assessed against several human cancer cell lines including MCF-7 (ER positive breast cancer cell), MDA-MB231 (ER-ne...

[ 47 ] - QSAR Analysis for Some 1, 2-Benzisothiazol-3-one Derivatives as Caspase-3 Inhibitors by Stepwise MLR Method

Caspase-3, one of the dominant effectors caspases, is activated in almost every model of apoptosis with various signaling pathways. Hence, inhibition of caspase-3 has become an attractive target in the treatment of neurodegenerative diseases. Caspase-3 inhibitory activities of some 1,2-benzisothiazol-3-one derivatives were modeled by quantitative structure–activity relationship (QSAR) using ste...

[ 48 ] - Design, Synthesis and Biological Evaluation of4-(Imidazolylmethyl)-2-(4-methylsulfonyl phenyl)-Quinoline Derivatives as Selective COX-2 Inhibitors and In-vitro Anti-breast Cancer Agents

A new group of 4-(Imidazolylmethyl) quinoline derivatives possessing a methylsulfonyl COX-2 pharmacophore at the para position of the C-2 phenyl ring were designed and synthesized as selective COX-2 inhibitors and in-vitro anti breast cancer agents. In-vitro COX-1 and COX-2 inhibition studies showed that all the compounds were potent and selective inhibitors of the COX-2 isozyme with IC50 value...

[ 49 ] - Development and Validation of an HPLC Method for Determination of Amifostine and/or Its Metabolite (WR-1065) In Human Plasma Using OPA Derivatization and UV Detection

A rapid, sensitive and reproducible HPLC method was developed and validatedfor the analysis of amifostine (AMF) and/or its metabolite, WR-1065 inhuman plasma. The method involves the alkylation of free sulfydryl group with iodoacetic acid followed by derivatization of the drug and its metabolite witho-phthaldialdehyde (OPA) andUVdetection at 340 nm. The derivatized AMF and WR-1065 were eluted i...

[ 50 ] - Design, Synthesis and Biological Evaluation of new 1,4-Dihydropyridine (DHP) Derivatives as Selective Cyclooxygenase-2 Inhibitors

As a continuous research for discovery of new COX-2 inhibitors, chemical synthesis, in vitro biological activity and molecular docking study of anew group of 1,4-dihydropyridine (DHP) derivatives were presented. Novel synthesized compounds possessing a COX-2 SO2Me pharmacophore at the para position of C-4 phenyl ring, different hydrophobic groups (R1) at C-2 position and alkoxycarbonyl groups (...

[ 51 ] - QSAR Study on Anti-HIV-1 Activity of 4-Oxo-1,4-dihydroquinoline and 4-Oxo-4H-pyrido[1,2-a]pyrimidine Derivatives Using SW-MLR, Artificial Neural Network and Filtering Methods

Predictive quantitative structure–activity relationship was performed on the novel 4-oxo-1,4-dihydroquinoline and 4-oxo-4H-pyrido[1,2-a]pyrimidine derivatives to explore relationship between the structure of synthesized compounds and their anti-HIV-1 activities. In this way, the suitable set of the molecular descriptors was calculated and the important descriptors using the variable selections ...

[ 52 ] - Design, Synthesis and Cytotoxicity Evaluationof New 1,2-diaryl-4, 5, 6, 7-Tetrahydro-1H-benzo[d] Imidazolesas Tubulin Inhibitors

A new series of 1,2-diaryl-4,5,6,7-tetrahydro-1H-benzo[d]imidazoles, possessing trimethoxy phenyl pharmacophore, were synthesized to evaluate their biological activities as tubulin inhibitors. Cytotoxic activity of the synthesized compounds 7a-f was assessed against several human cancer cell lines, including MCF-7 (breast cancer cell), HEPG2 (liver hepatocellular cells), A549 (adenocarcinomic h...

[ 53 ] - In-silico Investigation of Tubulin Binding Modes of a Series of Novel Antiproliferative Spiroisoxazoline Compounds Using Docking Studies

Interference with microtubule polymerization results in cell cycle arrest leading to cell death. Colchicine is a well-known microtubule polymerization inhibitor which does so by binding to a specific site on tubulin. A set of 3',4'-bis (substituted phenyl)-4'H-spiro[indene-2,5'-isoxazol]-1(3H)-one derivatives with known antiproliferative activities were evaluated for their tubulin binding modes...

[ 54 ] - Search for the Pharmacophore of Histone Deacetylase Inhibitors Using Pharmacophore Query and Docking Study

Histone deacetylase inhibitors have gained a great deal of attention recently for the treatment of cancers and inflammatory diseases. So design of new inhibitors is of great importance in pharmaceutical industries and labs. Creating pharmacophor models in order to design new molecules or search a library for finding lead compounds is of great interest. This approach reduces the overall cost ass...

[ 55 ] - Cytotoxicity of Selected Novel Chalcone Derivatives on Human Breast, Lung and Hepatic Carcinoma Cell Lines

Cancer is considered as a challenging deathly disease and discovering or synthesis of new cytotoxic agents is a worldwide attempt. In this study, a group of recently synthesized chalcones, with the structure of 1,3-diarylprop-2-en-1-one having differesnt COX-1 and/or COX-2 selectivities, have been examined on human hepatocarcinoma (HepG2), lung carcinoma (A549), and breast adenocarcinoma (MCF-7...

[ 56 ] - Design, Synthesis and Biological Evaluation of 5-Oxo-1,4,5,6,7,8 Hexahydroquinoline Derivatives as Selective Cyclooxygenase-2 Inhibitors

A group of regioisomeric 5-oxo-1,4,5,6,7,8 hexahydroquinoline derivatives possessing a COX-2 SO2Me pharmacophore at the para position of the C-2 or C-4 phenyl ring, in conjunction with a C-4 or C-2 phenyl (4-H) or substituted-phenyl ring (4-F,4-Cl,4-Br,4-OMe,4-Me, 4-NO2), were designed for evaluation as selective cyclooxygenase-2 (COX-2) inhibitors. These target 5-oxo-1,4,5,6,7,8 hexahydroquino...

[ 57 ] - Design, Synthesis and Cytotoxicity Evaluation of New 2-Aryl-5,6-Dihydropyrrolo[2, 1-a]Isoquinoline Derivatives as Topoisomerase Inhibitors

Two set of 2-aryl-5,6-dihydropyrrolo[2,1-a] isoquinolines were designed and synthesized to evaluate their biological activities as topoisomerase inhibitors. Cytotoxic activity of the synthesized compounds 4a-e and 7a-d was assessed against several human cancer cell lines, including MCF-7 (breast cancer cell), HepG2 (liver hepatocellular cells), A549 (adenocarcinomic human alveolar basal epithel...

[ 58 ] - Occurrence of Deoxynivalenol in Foods for Human Consumption from Tehran, Iran

AbstractThe occurrence of deoxynivalenol (DON) in retail foods in Tehran (Iran) was determined using high-performance liquid chromatography technique and immunoaffinity column as the clean-up step. A method was validated for analysis of DON in rice, bread, puffed corn snack and wheat flour. The average recoveries and precision (RSD) for DON in different foods ranged 84.2-93.1% and 2.9-12.0%, re...

[ 59 ] - Rapid High Performance Liquid Chromatographic Method for Determination of Clarithromycin in Human Plasma Using Amperometric Detection: Application in Pharmacokinetic and Bioequivalence Studies

A rapid, sensitive and reproducible HPLC method using amperometric detector was developed and validated for the analysis of clarithromycin in human plasma. The separation was achieved on a monolithic silica column (MZ- C8 125×4.0 mm) using acetonitrile- methanol-potassium dihydrogen phosphate buffer (40:6:54,v/v), with pH of 7.5, as the mobile phase at a flow rate of 1.5 mL/min. The assay enabl...

[ 60 ] - Improvement of Capillary Electrophoretic Enantioseparation of Fluoxetine by a Cationic Additive

One of the problems encountered in CE separations of basic compounds is the adsorption of analytes onto the negatively charged capillary wall which could lead to poor repeatability of migration time and peak area. Additionally, separation of enantiomers of chiral of basic drugs is commonly carried out in low pH buffer which contributes to strong ionic interaction of the cationic drug ions with ...

[ 61 ] - Analysis of Aflatoxin B1 in Iranian Foods Using HPLC and a Monolithic Column and Estimation of its Dietary Intake

A high performance liquid chromatographic method was developed for determination of aflatoxin B1 (AFB1) in foods using a monolithic column with sample clean up on an immunoaffinity column. The method was validated for analysis of AFB1 in rice, bread, puffed corn snack, wheat flour and peanut samples. The average recoveries for AFB1 in different foods ranged from 94.4 to 102.5% with the coeffici...

[ 62 ] - Evaluation of Anti-nociceptive and Anti-inflammatory Activities of Novel Chalcone Derivatives

Chalcone (1,3-diarylprop-2-en-1-one) derivatives have been introduced as selective cyclooxygenase-2 inhibitors. In the present study, anti-nociceptive and anti-inflammatory effects of eight novel compounds were evaluated in male mice and Wistar rats by using the writhing and formalin-induced paw edema tests respectively. The activities of the compounds were compared with celecoxib as a referenc...

[ 63 ] - Physical and Chemical Stability of Mycophenolate Mofetil (MMF) Suspension Prepared at the Hospital

To evaluate the physical and chemical stability of a suspension of mycophenolate mofetil (MMF) prepared in the hospital from commercially available MMF capsules and tablets. Extemporaneous pharmacy was used as a feasible method in this experimental study to prepare suspension form of MMF. Suspension formulations were prepared from both tablets and capsules forms of MMF. Thereafter the stability...

[ 64 ] - Exposure Assessment of the Tehran Population (Iran) to Zearalenone Mycotoxin

Zearalenone (ZEA) mycotoxin is a potent estrogenic metabolite. It is the primary toxin causing infertility, abortion or other breeding problems. A HPLC method was validated for ZEA in foods using a monolithic column with sample clean-up on an immunoaffinity column. A certified reference material (CRM) from FAPAS (UK) was analyzed. A survey of ZEA was performed on the 72 samples of rice, bread, ...

[ 65 ] - Selective COX-2 Inhibitors: A Review of Their Structure-Activity Relationships

Non-steroidal anti-inflammatory drugs (NSAIDs) are the competitive inhibitors of cyclooxygenase (COX), the enzyme which mediates the bioconversion of arachidonic acid to inflammatory prostaglandins (PGs). Their use is associated with the side effects such as gastrointestinal and renal toxicity. The therapeutic anti-inflammatory action of NSAIDs is produced by the inhibition of COX-2, while the ...

[ 66 ] - Synthesis and Cytotoxic Evaluation of Some Novel Sulfonamide Derivatives Against a Few Human Cancer Cells

Sulfonamides are the first effective chemotherapeutic agents used for several years to cure or prevent systemic bacterial infections. In addition, this agents showed anti-carbonic anhydrase and cause cell cycle perturbation in the G1 phase, disruption of microtubule assembly, suppression of the transcription activator Nf-Y, angiogenesis and matrix metalloproteinase (MMP). In recent years, novel...

[ 67 ] - Quantification of Polyethylene Glycol Esters of Methotrexate and Determination of Their Partition Coefficients by Validated HPLC Methods

Conjugation of methotrexate (MTX) (MW 454) with different molecular weights of polyethylene glycol (PEG) including methoxy-peg (mpeg) 750 D and 5000 D and diol-peg 35000 D led to compounds that are physicochemically highly different from the parent compound, MTX. In this study, an HPLC system consisting of C8 column and UV detector (?=342 nm), using a mixture of 30:70 v/v phosphate-citrate buff...

[ 68 ] - The Pharmacological Effects of Odonthobuthus doriae Scorpion Venom and Its Extracted Fractions on Neuro-Muscular Transmission

The effect of Odonthobuthos doriae (O.d) scorpion venom at 0/3, 1 and 3, 10 µg/ml concentrations were investigated on nerve-muscle transmission, using the Twitch tension technique. A concentration of 0.3 µg/ml caused a small change in the twitch height in response to indirect muscle stimulation, but higher concentrations (1, 3, 10 µg/ml) caused a transient augmentation in twitch response follow...

[ 69 ] - Rapid High Performance Liquid Chromatographic Determination of Risperidone in Human Plasma

A simple, rapid and sensitive high-performance liquid chromatographic (HPLC) method for the determination of risperidone in human plasma was developed. An HPLC system based on a Nucleosil C8 column (150?4 mm) and a UV detector (?= 280 nm) were used. A mixture of sodium dihydrogen phosphate buffer-acetonitrile (55:45, v/v) adjusted to pH 6.0 at a flow rate of 1.5 ml min-1 was used as mobile phas...

[ 70 ] - Survey of fumonisin B1 contamination of cornin Northern Iran during 2000

Fumonisin B1 (FB1) is the most abundant of the fumonisin mycotoxins, mainly produced in corn by fungi of the genus Fusarium. FB1 has been shown to be hepatocarcinogenic and nephrocarcinogenic in animals. Contamination of corn with FB1 was assayed in samples collected from Mazandaran Province, situated on the Caspian littoral of Iran, in September 2000. In this survey, 38 corn samples were analy...

[ 71 ] - Design and Synthesis of New Imidazole Derivatives of Captopril

A new series of alkylthio imidazole analogues of captopril, an ACE inhibitor used in the treatment of hypertension, was designed and synthesized in order to obtain agents more active than captopril with less side effects. All the compounds thus prepared were purified and characterized by IR, NMR and Mass analytical instruments.

[ 72 ] - Enhancement of percutaneous absorption of curcumin (turmeric pigment) by ethanol

Curcumin is the active component of Curcuma species including C. longa (turmeric). This molecule is well known for its anti-inflammatory effect, which seems to be stronger than that of hydrocortisone. Curcuma species have been used in Asian traditional medicine as topical anti-inflammatory drugs. Curcumin has poor oral bioavailability and its topical application could be of choice, particularly...

[ 73 ] - Separation of Somatropin and Its Degradation Products by High-Performance Liquid Chromatography Using a Reversed-Phase Polymeric Column

The accurate prediction of protein stability is one of the most challenging goals in protein formulation and delivery. In this study, a gradient RP-HPLC method is described for the separation of human growth hormone (hGH) variants as deamidated and oxidized forms. The methodology employed a polymeric poly (styrene-co-divinylbenzene) column and a 1mL/min flow rate of a linear gradient of 0.1% v/...

[ 74 ] - Stereoselective Permeation of Tretinoin and Isotretinoin through Enhancer-Treated Rat Skin. II. Effects of Lipophilic Penetration Enhnacers

Many properties of chemicals depend on their stereochemistry. Among these, the effects of stereoisomerism on percutaneous absorption of drugs are not well studied. We have previously shown that permeation of tretinoin and isotretinoin (two geometric isomers) through hydrophilic enhancers-treated rat skin is stereoselective. As, depending on their lipophilicity, penetration enhancers can change ...

[ 75 ] - Stereoselective Permeation of Tretinoin and Isotretinoin through Enhancer-Treated Rat Skin. I. Effect of Ethanol and Sodium Dodecyl Sulfate

Many properties of chemicals depend on their streochemistry. Among these, the effects of streoisomerism on percutaneous absorption of drugs, which is subject of the present investigation, is not well studied yet. In this study, tretinoin (TT) and isotretinoin (ITT) (geometric isomers) were chosen and their permeations (alone or in the presence of each other) through enhancer-treated excised ...

[ 76 ] - Bioequivalence Studies of Two Formulations of Baclofen Tablet in Healthy Volunteers

The relative bioavailability of the test (generic) product 2 × 25 mg baclofen tablets, with respect to the reference product, Lioresal® 2 × 25 mg tablets (baclofen; Squibb) was determined in a single-blind, single dose, randomised, crossover study. The mean values for the variable Cmax were 737.6 ng/ml for the reference and 739.5 ng/ml for the test product. The mean values for the variable AUC ...

[ 77 ] - A Modified Method for the Synthesis of Nitrofurazone

Nitrofurazone is one of the antibacterial nitrofuran agents used topically for skin infections. The drug is effective on the majority of infectious microorganisms. Because of the importance of this drug in clinic, in this study various methods of synthesis of nitrofurazone were examined and the most appropriate method, applicable to pharmaceutical industry was chosen and optimized from the poin...

[ 78 ] - Synthesis and Biological Evaluation of New 1, 4-Dihydropyridines as Antihypertensives Agents in Rats

New analogues of nifedipine, as a known calcium channel blocker, were synthesized by replacing the orthonitrophenyl group on position 4 with 1-(4-Nitrobenzyl)-5-imidazolyl or 2-methylthio-1-(4-Nitrobenzyl)-5-imidazolyl substituent. Effects of the new synthesized compounds on blood pressure were studied at 15, 30 and 60 min after administration by indirect tail-cuff method and compared with nife...

[ 79 ] - Synthesis, Characterization and In-vitro Evaluation of Novel Naphthoquinone Derivatives and Related Imines: Identification of New Anticancer Leads

Quinones such as 1,4-naphthoquinones are abundant in nature and naphthoquinone based natural products are known to possess anticancer activity. This pharmacophore is known to convey anticancer activity to some drugs such as streptonigrin, mitomycin A, etc. We synthesized and characterized different classes of naphthoquinone derivatives including bis naphthoquinone, 2-arylaminonaphthoquinone, be...

[ 80 ] - Design, Synthesis, Molecular Modeling, In Silico ADME Studies and Anti-HIV-1 Assay of New Diazocoumarin Derivatives

Some new diazo incorporated coumarin compounds were designed and synthesized to evaluate their anti-HIV activity. Overall, compounds were active against HIV at 100 μM. Additionally, no cytotoxic effect was observed at this concentration. The compound with 4-chlorobenzyl group indicated the best anti-HIV activity (52%). Docking studies using the later crystallographic data available for PFV inte...

[ 81 ] - Design, Synthesis and Biological Evaluation of New Imidazo[2,1-b]Thiazole Derivatives as Selective COX-2 Inhibitors

A new series of imidazo[2,1-b]thiazole analogs containing a methyl sulfonyl COX-2 pharmacophore was synthesized and evaluated for their COX-2 inhibitory activity. According to in-vitro COX-1/COX-2 inhibition data, all compounds (6a-g) were selective inhibitors of COX-2 isoenzyme with IC50 values in the highly potent 0.08-0.16 mM range. These results indicated that both potency and selectivity o...

[ 82 ] - Design, Synthesis and Biological Evaluation of Ketoprofen Conjugated To RGD/NGR for Targeted Cancer Therapy

It is well known that Arginine-Glycine-Aspartic acid (RGD) and Asparagine-Glycine-Arginine (NGR) peptides preferentially bind to integrin receptors and aminopeptidase Nrespectively and these two receptors play important roles in angiogenesis. Therefore ketoprofenas a non-selective cox Inhibitor was conjugated with linear RGD and NGR to take advantageof targeting capability of these two motifs a...

[ 83 ] - Novel Colchicine Analogues Target Mitochondrial PT Pores Using Free Tubulins and Induce ROS-Mediated Apoptosis in Cancerous Lymphocytes

B-acute lymphoblastic leukemia (B-ALL) is the frequent pediatric malignity. Chemotherapy is the most practical approaches to deal with such malignancies. Microtubule-targeted agents are one of the most strategic drugs which formerly use in chemotherapy.Although,colchicine-binding anti-tubulin agents exhibited promising effects in clinical trials, their exact mechanism of action is not fully und...

[ 84 ] - Synthesis, Characterization and In-vitro Evaluation of Novel Naphthoquinone Derivatives and Related Imines: Identification of New Anticancer Leads

Quinones such as 1,4-naphthoquinones are abundant in nature and naphthoquinone based natural products are known to possess anticancer activity. This pharmacophore is known to convey anticancer activity to some drugs such as streptonigrin, mitomycin A, etc. We synthesized and characterized different classes of naphthoquinone derivatives including bis naphthoquinone, 2-arylaminonaphthoquinone, be...

[ 85 ] - Design, Synthesis, Molecular Modeling, In Silico ADME Studies and Anti-HIV-1 Assay of New Diazocoumarin Derivatives

Some new diazo incorporated coumarin compounds were designed and synthesized to evaluate their anti-HIV activity. Overall, compounds were active against HIV at 100 μM. Additionally, no cytotoxic effect was observed at this concentration. The compound with 4-chlorobenzyl group indicated the best anti-HIV activity (52%). Docking studies using the later crystallographic data available for PFV inte...

[ 86 ] - Design, Synthesis and Biological Evaluation of New Imidazo[2,1-b]Thiazole Derivatives as Selective COX-2 Inhibitors

A new series of imidazo[2,1-b]thiazole analogs containing a methyl sulfonyl COX-2 pharmacophore was synthesized and evaluated for their COX-2 inhibitory activity. According to in-vitro COX-1/COX-2 inhibition data, all compounds (6a-g) were selective inhibitors of COX-2 isoenzyme with IC50 values in the highly potent 0.08-0.16 mM range. These results indicated that both potency and selectivity o...

[ 87 ] - Design, Synthesis and Biological Evaluation of Ketoprofen Conjugated To RGD/NGR for Targeted Cancer Therapy

It is well known that Arginine-Glycine-Aspartic acid (RGD) and Asparagine-Glycine-Arginine (NGR) peptides preferentially bind to integrin receptors and aminopeptidase Nrespectively and these two receptors play important roles in angiogenesis. Therefore ketoprofenas a non-selective cox Inhibitor was conjugated with linear RGD and NGR to take advantageof targeting capability of these two motifs a...

[ 88 ] - Novel Colchicine Analogues Target Mitochondrial PT Pores Using Free Tubulins and Induce ROS-Mediated Apoptosis in Cancerous Lymphocytes

B-acute lymphoblastic leukemia (B-ALL) is the frequent pediatric malignity. Chemotherapy is the most practical approaches to deal with such malignancies. Microtubule-targeted agents are one of the most strategic drugs which formerly use in chemotherapy.Although,colchicine-binding anti-tubulin agents exhibited promising effects in clinical trials, their exact mechanism of action is not fully und...

[ 89 ] - Colchicine-like β-acetamidoketones as inhibitors of microtubule polymerization: Design, synthesis and biological evaluation of in vitro anticancer activity

Objective(s): In this study a series of novel colchicine-like β-acetamidoketones was designed and synthesized as potential tubulin inhibitorsMaterials and Methods: The cytotoxicity of the novel synthesized β-acetamidoketones was assessed against two cancerous cell lines including MCF-7 (human breast cancer cells) and A549 (adenocarcinomi...

[ 90 ] - Molecular Docking and QSAR Study of 2-Benzoxazolinone, Quinazoline and Diazocoumarin Derivatives as Anti-HIV-1 Agents

A series of 2-benzoxazolinone, diazocoumarin and quinazoline derivatives have been shown to inhibit HIV replication in cell culture. To understand the pharmacophore properties of selected molecules and design new anti-HIV agents, quantitative structure–activity relationship (QSAR) study was developed using a descriptor selection approach based on the stepwise method. Multiple linear regression ...

[ 91 ] - Investigating the Antimicrobial Efficacy of Liposomal Vancomycin in Gram-positive and Gram-negative bacteria- A Preliminary Mechanistic Study

Outer membrane of Gram-negative bacteria is a permeability barrier to many antibacterial agents, including the glycopeptide antibiotics such as vancomycin hydrochloride and as a result these antibiotics are ineffective against Gram negative bacteria. Different strategies have been described to overcome such limitation, including application of nanoparticles, as was shown in our previous studies...

[ 92 ] - Molecular Docking and QSAR Study of 2-Benzoxazolinone, Quinazoline and Diazocoumarin Derivatives as Anti-HIV-1 Agents

A series of 2-benzoxazolinone, diazocoumarin and quinazoline derivatives have been shown to inhibit HIV replication in cell culture. To understand the pharmacophore properties of selected molecules and design new anti-HIV agents, quantitative structure–activity relationship (QSAR) study was developed using a descriptor selection approach based on the stepwise method. Multiple linear regression ...

[ 93 ] - Design, Synthesis, Molecular Modeling Studies and Biological Evaluation of N'-Arylidene-6-(benzyloxy)-4-oxo-1,4-dihydroquinoline-3-carbohydrazide Derivatives as Novel Anti-HCV Agents

HCV-induced hepatitis is one of the most debilitating diseases. The limited number of anti-HCV drugs and drug-resistance necessitate developing of new scaffolds with different mode of actions. HCV non-structural protein 5B (NS5B) is an attractive target for development of novel inhibitors of HCV replication. In this paper, new N'-arylidene-6-(benzyloxy)-4-oxo-1,4-dihydroquinoline-3-carbohydrazi...

[ 94 ] - Design, Synthesis, Molecular Modeling Studies and Biological Evaluation of N'-Arylidene-6-(benzyloxy)-4-oxo-1,4-dihydroquinoline-3-carbohydrazide Derivatives as Novel Anti-HCV Agents

HCV-induced hepatitis is one of the most debilitating diseases. The limited number of anti-HCV drugs and drug-resistance necessitate developing of new scaffolds with different mode of actions. HCV non-structural protein 5B (NS5B) is an attractive target for development of novel inhibitors of HCV replication. In this paper, new N'-arylidene-6-(benzyloxy)-4-oxo-1,4-dihydroquinoline-3-carbohydrazi...

[ 95 ] - Design, Synthesis, Molecular Modeling Study and Biological Evaluation of New N'-arylidene-pyrido[2,3-d]pyrimidine-5-carbohydrazide Derivatives as Anti-HIV-1 Agents

In an attempt to identify potential new agents that are active against HIV-1, a series of novel pyridopyrimidine-5-carbohydrazide derivatives featuring a substituted benzylidene fragment were designed and synthesized based on the general pharmacophore of HIV-1 integrase inhibitors. The cytotoxicity profiles of these compounds showed no significant toxicity to human cells and they exhibited anti...

[ 96 ] - Design, Synthesis, Molecular Modeling Study and Biological Evaluation of New N'-arylidene-pyrido[2,3-d]pyrimidine-5-carbohydrazide Derivatives as Anti-HIV-1 Agents

In an attempt to identify potential new agents that are active against HIV-1, a series of novel pyridopyrimidine-5-carbohydrazide derivatives featuring a substituted benzylidene fragment were designed and synthesized based on the general pharmacophore of HIV-1 integrase inhibitors. The cytotoxicity profiles of these compounds showed no significant toxicity to human cells and they exhibited anti...

[ 97 ] - Naringenin Enhances the Anti-Cancer Effect of Cyclophosphamide against MDA-MB-231 Breast Cancer Cells Via Targeting the STAT3 Signaling Pathway

Naringenin is a natural compound with potential anti-cancer effects against several cancer types. Also, its precise molecular mechanisms regarding tumor growth suppression has not been completely elucidated. In the current study the apoptosis-inducing and anti-proliferative effects of Naringenin together with cyclophosphamide were studied in breast cancer cells and the participation of JAK2/ST...

[ 98 ] - Naringenin Enhances the Anti-Cancer Effect of Cyclophosphamide against MDA-MB-231 Breast Cancer Cells Via Targeting the STAT3 Signaling Pathway

Naringenin is a natural compound with potential anti-cancer effects against several cancer types. Also, its precise molecular mechanisms regarding tumor growth suppression has not been completely elucidated. In the current study the apoptosis-inducing and anti-proliferative effects of Naringenin together with cyclophosphamide were studied in breast cancer cells and the participation of JAK2/ST...