Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry, Pharmaceutical Sciences and Computational Chemistry
ISSN: 0975-413X
Abstract
Antiglycation and anticancer activity of some newer synthetic flavones
Author(s): Jayashree B. S, Piyush Chaturvedi, Venkatachalam H, P V R Chaudary, Yogendra NayakFlavonoids have been used for prevention and treatment for diabetes and cancer.Several attempts have been made earlier to substitute the γ-benzopyronepharmacophore in the flavonoid ring. We have substituted α-position in the γ- benzopyrone ring with a thiophenyl group.Thus the newer chalcones (JPC-1 and JPC-19), 3-hydroxy flavones (JPC- 2 and JPC-20) and many new substituted 3-benzyloxy derivatives of flavones were synthesized, purified, characterized by their spectral studies, and their logs P, εmaxvalues were determined. The synthesized compounds were screened for in vitro antiglycation and anticancer activities. In the in vitroglycosylation usinghaemoglobinglucose method, test compounds JPC-6 and JPC-10 showed activity less than 100μg/ml when compared to that of α- tocopherol acetate. All the other test compounds showed antiglycation activity more than 100μg/ml.In the BSAglucose assay, JPC-8 showed antiglycation activity less than100 μg/mland was comparable to quercetin. Test compounds JPC-10 and JPC-13 showed significant in vitroanticancer activity with IC50values 43.50 and 67.44 μg/ml respectively, when they were tested on Ehrlich’s Ascitic Carcinoma (EAC)cells by trypan blue exclusion assay.
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