Optimization of the aromatase inhibitory activities of pyridylthiazole analogues of resveratrol

AS Mayhoub, L Marler, TP Kondratyuk, EJ Park…

Index: Mayhoub, Abdelrahman S.; Marler, Laura; Kondratyuk, Tamara P.; Park, Eun-Jung; Pezzuto, John M.; Cushman, Mark Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 7 p. 2427 - 2434

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Citation Number: 18

Abstract

Aromatase is an established target not only for breast cancer chemotherapy, but also for breast cancer chemoprevention. The moderate and non-selective aromatase inhibitory activity of resveratrol (1) was improved about 100-fold by replacement of the ethylenic bridge with a thiadiazole and the phenyl rings with pyridines (eg, compound 3). The aromatase inhibitory activity was enhanced over 6000-fold by using a 1, 3-thiazole as the central ring ...