Design, synthesis, and biological evaluation of (E)-and (Z)-styryl-2-acetoxyphenyl sulfides and sulfones as cyclooxygenase-2 inhibitors

…, VR Pallela, P Venkatapuram, R Boominathan…

Index: Reddy, M.V. Ramana; Mallireddigari, Muralidhar Reddy; Pallela, Venkat R.; Venkatapuram, Padmavathi; Boominathan, Rengasamy; Bell, Stanley C.; Reddy, E. Premkumar Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 5 p. 1715 - 1723

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Citation Number: 23

Abstract

A new series of styryl acetoxyphenyl sulfides and sulfones possessing (E)-and (Z)- configurations were designed and prepared by stereospecific syntheses. All these compounds were evaluated for their ability to inhibit COX-2 enzyme in vitro. Structure– activity relationship studies on these compounds revealed that only sulfides with (Z)- configuration have potential COX-2 inhibitory activity. This inactivation of the enzyme is ...