In-silico quantitative structure-activity relationship (QSAR) study was performed to develop a model on series of novel pyrazole derivatives containing acetamide moiety which exhibited considerable antiproliferative activity against human colorectal adenocarcinoma cell line HT-29. The obtained has correlation coefficient (r) 0.9693, squared (r2) 0.9395 and leave-one-out (LOO) cross-validation (...

BACKGROUND AND PURPOSE Pyrazole derivatives have recently been suggested as selective blockers of transient receptor potential cation (TRPC) channels but their ability to distinguish between the TRPC and Orai pore complexes is ill-defined. This study was designed to characterize a series of pyrazole derivatives in terms of TRPC/Orai selectivity and to delineate consequences of selective suppres...

A series of curcumin pyrazole derivatives (3a-3e) were investigated for in-vitro hypolipidemic activity. The compounds were screened for the inhibition studies of the enzymes such as pancreatic lipase, glucose 6 phosphate dehydrogenase and malate dehydrogenase which are actively involved in lipid metabolism. Curcumin and all the other compounds in the series showed differential enzyme inhibitor...

Department of Pharmaceutical technology, Meerut Institute of Engineering and Technology, Meerut. ABSTRACT Pyrazole and pyrimidine derivatives attracted organic chemists due to their various biological and chemotherapeutic significance. Pyrazolopyrimidines and related fused heterocycles are of important as probable bioactive molecules. The heterocyclic fusion of pyrimidine ring and pyrazole ring...

Flavonoids comprise a large family of plant derived polyphenolic compounds classified as flavonols, chalcones, aurones, flavanones, isoflavones, flavans, flavanonols, flavanols, and flavones differencing from each other in their structural group arrangements [1]. α,β-Unsaturated ketones display a wide range of pharmacological properties, including cytotoxicity towards different cancer cell line...

A series of novel aryl-2H-pyrazole derivatives bearing 1,4-benzodioxan or 1,3-benzodioxole moiety were designed as potential telomerase inhibitors to enhance the ability of aryl-2H-pyrazole derivatives to inhibit telomerase, a target of anticancer. The telomerase inhibition tests showed that compound 16A displayed the most potent inhibitory activity with IC(50) value of 0.9 μM for telomerase. T...