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

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

文献索引：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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被引用次数: 84

摘要

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 ...