Benzothiophene selective estrogen receptor modulators with modulated oxidative activity and receptor affinity

Z Qin, I Kastrati, REP Chandrasena, H Liu…

Index: Qin, Zhihui; Kastrati, Irida; Chandrasena, R. Esala P.; Liu, Hong; Yao, Ping; Petukhov, Pavel A.; Bolton, Judy L.; Thatcher, Gregory R. J. Journal of Medicinal Chemistry, 2007 , vol. 50, # 11 p. 2682 - 2692

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Citation Number: 84

Abstract

The regulation of estrogenic and antiestrogenic effects of selective estrogen receptor modulators (SERMs) is thought to underlie their clinical use. Most SERMs are polyaromatic phenols susceptible to oxidative metabolism to quinoids, which are proposed to be genotoxic. Conversely, the redox reactivity of SERMs may contribute to antioxidant and chemopreventive mechanisms, providing a new approach to improve the therapeutic ...