Synthesis and Structure-Activity Relationship of Novel 6-Aryl-1, 4-dihydrobenzo [d][1, 3] oxazine-2-thiones as Progesterone Receptor Modulators Leading to the …

A Fensome, R Bender, R Chopra, J Cohen…

Index: Fensome, Andrew; Bender, Reinhold; Chopra, Rajiv; Cohen, Jeff; Collins, Mark A.; Hudak, Valerie; Malakian, Karl; Lockhead, Susan; Olland, Andrea; Svenson, Kristine; Terefenko, Eugene A.; Unwalla, Ray J.; Wilhelm, James M.; Wolfrom, Scott; Zhu, Yuan; Zhang, Zhiming; Zhang, Puwen; Winneker, Richard C.; Wrobel, Jay Journal of Medicinal Chemistry, 2005 , vol. 48, # 16 p. 5092 - 5095

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Citation Number: 69

Abstract

Tanaproget represents a potential first-in-class nonsteroidal PR agonist for contraception with improved safety and side effect profiles versus currently available steroidal oral contraceptives. Additional SAR, biological activity, and structural information from a tanaproget/hPR-LBD (hPR-LBD= human progesterone receptor ligand binding domain) cocrystal structure will also be presented.