Cytochrome P450 inhibition potential of Liv.52, snuff and camphor was assessed using human liver microsomes for any clinical consequences if taken together with other medications. They were screened for potential to inhibit 9 drug metabolizing cytochrome P450 (CYP 450) isoforms. Samples were analyzed by liquid chromatography mass spectrometry (LC-MS/MS) using stable labeled internal standards o...

Sulfonamide derivatives serve as an important building blocks in the drug design discovery and development (4D) process. Ciprofloxacin-, sulfadiazine- and amantadine-based sulfonamides were synthesized as potent inhibitors of jack bean urease and free radical scavengers. Molecular diversity was explored and electronic factors were also examined. All 24 synthesized compounds exhibited excellent ...

Inula species are medicinal and aromatic plants used for folk medicine extensively. In this work, hydrodistilled essential oil of Inula graveolens (Linnaeus) Desf. analyzed by GC-MS which revealed that bornyl acetate was the major product (69.15%). Camphene was the second major compound (11.11%). Antiproliferative activity of the essential oil and bornyl acetate was investigated on HeLa (human ...

Cancer is a major global problem and is the second leading cause of mortality in the developed countries.Resistance to current chemotherapeutics and high incidence of adverse effects are the two principal reasons for developing new anticancer agents. Phenylacetamide derivatives can act as potential anticancer agents. Synthesis and screening of 2-(4-Fluorophenyl)- N-phenylacetamide derivatives i...

The anti-Trypanosoma cruzi activity of 5-nitro-2-furfuriliden derivatives as well as the cytotoxicity of these compounds on J774 macrophages cell line and FN1 human fibroblast cells were investigated in this study. The most active compounds of series I and II were 4-butyl-[N'-(5-nitrofuran-2-yl) methylene] benzidrazide (3g; IC50=1.05μM±0.07) and 3-acetyl-5-(4-butylphenyl)-2-(5-nitrofuran-2-yl)-...

The endophytic fungus Fusarium equiseti was isolated from the brown alga Padina pavonica, collected from the Red Sea. The fungus was identified by its morphology and 18S rDNA. Cultivation of this fungal strain in biomalt-peptone medium led to isolation of 12 known metabolites of diketopeprazines and anthraquinones. The organic extract and isolated compounds were screened for their inhibition of...

Two classes of modified analogs of 4-(thiazol-5-yl)benzoic acid-type CK2 inhibitors were designed. The azabenzene analogs, pyridine- and pyridazine-carboxylic acid derivatives, showed potent protein kinase CK2 inhibitory activities [IC50 (CK2α)=0.014-0.017μM; IC50 (CK2α')=0.0046-0.010μM]. Introduction of a 2-halo- or 2-methoxy-benzyloxy group at the 3-position of the benzoic acid moiety maintai...

Thioredoxin reductase (TrxR) is an enzyme that involved in many metabolic pathways from detoxification to reduction of radicals by catalyzing the thioredoxin, and therefore associated with physiological processes, including cancer. Inhibitors this are considered anticancer targets. In past studies, some antidepressants have been found effects through various mechanisms, reuse as drugs has attra...