Farzad Kobarfard

[ 1 ] - Novel and efficient method for solid phase synthesis of urea-containing peptides targeting prostate specific membrane antigen (PSMA) in comparison with current methods

The basic chemical structure of most prostate specific membrane antigen (PSMA) inhibitors which are now in pre-clinical and clinical studies is Glu-Ureido-based peptides. Synthesis of urea-based PSMA inhibitors includes two steps: 1- isocyanate intermediate formation and 2- urea bond formation. In current methods, isocyanate is formed in liquid phase and then reacts with amine existing in liqui...

[ 2 ] - Synthesis, Radiolabeling, and Biological Evaluation of Peptide LIKKPF Functionalized with HYNIC as Apoptosis Imaging Agent

Introduction: A noninvasive method of detecting exposure of phosphatidylserine (PS) on the external surface of the plasma membrane such as nuclear imaging could assist the diagnosis and therapy of apoptosis related pathologies. The most studied imaging agent for apoptosis is Annexin V so far. Because of limitations of Annexin V other agents have been introduced such as small peptides and molecu...

[ 3 ] - Synthesis, Antiplatelet Activity and Cytotoxicity Assessment of Indole-Based Hydrazone Derivatives

A series of indole-based aryl(aroyl)hydrazone analogs of antiplatelet indole-3-carboxaldehyde phenylhydrazone were synthesized by the Schiff base formation reaction and their antiplatelet activity was assessed using human platelet rich plasma. The platelet concentrate was obtained using a two-step centrifugation protocol and ADP, arachidonic acid and collagen were used as inducers of platelet a...

[ 4 ] - Determination of Mebudipine in Human Plasma by Liquid Chromatography–tandem Mass Spectrometry

In previous studies, mebudipine, a dihydropyridine calcium channel blocker, showed a considerable potential to be used in cardiovascular diseases. The aim of the current study was to develop a valid method using reversed-phase high performance liquid chromatography coupled with electrospray ionization mass spectrometry to assay mebudipine in the human plasma. Separation was achieved on a Zorbax...

[ 5 ] - Biotransformation of Progesterone by Whole Cells of Filamentous Fungi Aspergillus brasiliensis

Microbial steroid biotransformation have found wide-reaching application for the production of more precious and functionalized compounds due to their high regio-and stereoselectivity. In this study, the possibility of using filamentous fungi Aspergillus brasiliensis cells in the biotransformation of progesterone (I), a C-21 steroid hormone was studied for the first time.The fungal strain was i...

[ 6 ] - Variations in Intraplatelet Phospho-VASP Expression Due to Pre-analytical Sample Preparations, Illustration of a Quality Control Issue in Platelet Pharmacology

Intraplatelet phospho-VASP analysis is a commonly used approach for monitoring of anti-platelet therapy; however, testing of intraplatelet phospho-VASP expression needs a high level of experience and proficiency. The ability to recognize how the pre-analytical variations can change the results would be helpful for the interpretation of data from intraplatelet P-VASP analysis. The aim of this st...

[ 7 ] - Synthesis, Evaluation of Anticancer Activity and QSAR Study of Heterocyclic Esters of Caffeic Acid

Caffeic acid phenethyl ester(CAPE) suppresses the growth of transformed cells such as human breast cancer cells, hepatocarcinoma , myeloid leukemia, colorectal cancer cells, fibrosarcoma, glioma and melanoma. A group of heterocyclic esters of caffeic acid was synthesized using Mitsunobu reaction and the esters were subjected to further structural modification by electrooxidation of the catecho...

[ 8 ] - Synthesis and Molecular-cellular Mechanistic Study of Pyridine Derivative of Dacarbazine

Dacarbazine is an antitumor prodrug which is used for the treatment of malignant metastatic melanoma and Hodgkin’s disease. It requires initial activation in liver through an N-demethylationreaction. The active metabolite prevents the progress of disease via alkylation of guanine bases in DNA strands. In order to investigate the importance of imidazole ring and its dynamictautomerization in ant...

[ 9 ] - Electrochemical Synthesis of Novel 1,3-Indandione Derivatives and Evaluation of Their Antiplatelet Aggregation Activities

Electrochemical oxidation of some selected catechol derivatives, using cyclic voltammetry, in the presence of different 2-aryl-1,3-indandiones as nucleophiles, resulted in electrochemical synthesis of new 1,3- indandione derivatives in an undivided cell in good yield and purity. A Michael addition mechanism was proposed for the formation of the analogs based on the reaction conditions which wer...

[ 10 ] - Novel and efficient method for solid phase synthesis of urea-containing peptides targeting prostate specific membrane antigen (PSMA) in comparison with current methods

The basic chemical structure of most prostate specific membrane antigen (PSMA) inhibitors which are now in pre-clinical and clinical studies is Glu-Ureido-based peptides. Synthesis of urea-based PSMA inhibitors includes two steps: 1- isocyanate intermediate formation and 2- urea bond formation. In current methods, isocyanate is formed in liquid phase and then reacts with amine existing in liqui...

[ 11 ] - Synthesis, Radiolabeling, and Biological Evaluation of Peptide LIKKPF Functionalized with HYNIC as Apoptosis Imaging Agent

Introduction: A noninvasive method of detecting exposure of phosphatidylserine (PS) on the external surface of the plasma membrane such as nuclear imaging could assist the diagnosis and therapy of apoptosis related pathologies. The most studied imaging agent for apoptosis is Annexin V so far. Because of limitations of Annexin V other agents have been introduced such as small peptides and molecu...

[ 12 ] - Synthesis, Antiplatelet Activity and Cytotoxicity Assessment of Indole-Based Hydrazone Derivatives

A series of indole-based aryl(aroyl)hydrazone analogs of antiplatelet indole-3-carboxaldehyde phenylhydrazone were synthesized by the Schiff base formation reaction and their antiplatelet activity was assessed using human platelet rich plasma. The platelet concentrate was obtained using a two-step centrifugation protocol and ADP, arachidonic acid and collagen were used as inducers of platelet a...

[ 13 ] - Determination of Mebudipine in Human Plasma by Liquid Chromatography–tandem Mass Spectrometry

In previous studies, mebudipine, a dihydropyridine calcium channel blocker, showed a considerable potential to be used in cardiovascular diseases. The aim of the current study was to develop a valid method using reversed-phase high performance liquid chromatography coupled with electrospray ionization mass spectrometry to assay mebudipine in the human plasma. Separation was achieved on a Zorbax...

[ 14 ] - Biotransformation of Progesterone by Whole Cells of Filamentous Fungi Aspergillus brasiliensis

Microbial steroid biotransformation have found wide-reaching application for the production of more precious and functionalized compounds due to their high regio-and stereoselectivity. In this study, the possibility of using filamentous fungi Aspergillus brasiliensis cells in the biotransformation of progesterone (I), a C-21 steroid hormone was studied for the first time.The fungal strain was i...

[ 15 ] - Variations in Intraplatelet Phospho-VASP Expression Due to Pre-analytical Sample Preparations, Illustration of a Quality Control Issue in Platelet Pharmacology

Intraplatelet phospho-VASP analysis is a commonly used approach for monitoring of anti-platelet therapy; however, testing of intraplatelet phospho-VASP expression needs a high level of experience and proficiency. The ability to recognize how the pre-analytical variations can change the results would be helpful for the interpretation of data from intraplatelet P-VASP analysis. The aim of this st...

[ 16 ] - Synthesis, Evaluation of Anticancer Activity and QSAR Study of Heterocyclic Esters of Caffeic Acid

Caffeic acid phenethyl ester(CAPE) suppresses the growth of transformed cells such as human breast cancer cells, hepatocarcinoma , myeloid leukemia, colorectal cancer cells, fibrosarcoma, glioma and melanoma. A group of heterocyclic esters of caffeic acid was synthesized using Mitsunobu reaction and the esters were subjected to further structural modification by electrooxidation of the catecho...

[ 17 ] - Synthesis and Molecular-cellular Mechanistic Study of Pyridine Derivative of Dacarbazine

Dacarbazine is an antitumor prodrug which is used for the treatment of malignant metastatic melanoma and Hodgkin’s disease. It requires initial activation in liver through an N-demethylationreaction. The active metabolite prevents the progress of disease via alkylation of guanine bases in DNA strands. In order to investigate the importance of imidazole ring and its dynamictautomerization in ant...

[ 18 ] - Electrochemical Synthesis of Novel 1,3-Indandione Derivatives and Evaluation of Their Antiplatelet Aggregation Activities

Electrochemical oxidation of some selected catechol derivatives, using cyclic voltammetry, in the presence of different 2-aryl-1,3-indandiones as nucleophiles, resulted in electrochemical synthesis of new 1,3- indandione derivatives in an undivided cell in good yield and purity. A Michael addition mechanism was proposed for the formation of the analogs based on the reaction conditions which wer...

[ 19 ] - Optimization of RGD-modified Nano-liposomes Encapsulating Eptifibatide

Background: Eptifibatide (Integrilin) is an intravenous (IV) peptide drug that selectively inhibits ligand binding to the platelet GP IIb/IIIa receptor. It is an efficient peptide drug, however has a short half-life. Therefore, antithrombotic agents like eptifibatide are required to become improved with a protected and targeted delivery system such as using nano-liposomes to the site of thrombu...

[ 20 ] - 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...

[ 21 ] - 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...

[ 22 ] - RGD-Modified Nano-Liposomes Encapsulated Eptifibatide with Proper Hemocompatibility and Cytotoxicity Effect

Background: Eptifibatide (Integrilin®) is a hepta-peptide drug which specifically prevents the aggregation of activated platelets. The peptide drugs are encapsulated into nanolipisomes in order to decreasing their side effects and improving their half-life and bioavailability. Objectives: In this study, the in vitro cytotoxicity and hemocompatibi...

[ 23 ] - Validation of an Analytical Method for Simultaneous Determination of 18 Persistent Organic Pollutants in Trout Using LLE Extraction and GC-MS/MS

Persistent organic pollutants, (POPs), are vast distributed compounds in environment which are recognized as one of the global pollution problems. These groups of materials being dangerous due to their high stability are accumulated in animal tissues and occurring in the food chain. One of the major paths through which persistent organic combinations access to human body is consuming polluted f...

[ 24 ] - Optimization and High Level Production of Recombinant Synthetic Streptokinase in E. coli Using Response Surface Methodology

Streptokinase (SK) is an extracellular protein comprising 414 amino acids with considerable clinical importance as a commonly used thrombolytic agent. Due to its wide spread application and clinical importance designing more efficient SK production platforms worth investigatinginvestigation. In this regard, a synthetic SK gene was optimized and cloned in to pET21b plasmid for periplasmic expres...

[ 25 ] - Validation of an Analytical Method for Simultaneous Determination of 18 Persistent Organic Pollutants in Trout Using LLE Extraction and GC-MS/MS

Persistent organic pollutants, (POPs), are vast distributed compounds in environment which are recognized as one of the global pollution problems. These groups of materials being dangerous due to their high stability are accumulated in animal tissues and occurring in the food chain. One of the major paths through which persistent organic combinations access to human body is consuming polluted f...

[ 26 ] - Optimization and High Level Production of Recombinant Synthetic Streptokinase in E. coli Using Response Surface Methodology

Streptokinase (SK) is an extracellular protein comprising 414 amino acids with considerable clinical importance as a commonly used thrombolytic agent. Due to its wide spread application and clinical importance designing more efficient SK production platforms worth investigatinginvestigation. In this regard, a synthetic SK gene was optimized and cloned in to pET21b plasmid for periplasmic expres...