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. 2005 Aug 11;48(16):5092-5.
doi: 10.1021/jm050358b.

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 potent and selective nonsteroidal progesterone receptor agonist tanaproget

Andrew Fensome  1 , Reinhold Bender, Rajiv Chopra, Jeff Cohen, Mark A Collins, Valerie Hudak, Karl Malakian, Susan Lockhead, Andrea Olland, Kristine Svenson, Eugene A Terefenko, Ray J Unwalla, James M Wilhelm, Scott Wolfrom, Yuan Zhu, Zhiming Zhang, Puwen Zhang, Richard C Winneker, Jay Wrobel
Affiliations

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 potent and selective nonsteroidal progesterone receptor agonist tanaproget

Andrew Fensome et al. J Med Chem. .

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.

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