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; Reinhold H. W. Bender; Rajiv Chopra; Jeff Cohen; Mark A. Collins; Valerie Hudak; Karl Malakian; Susan Lockhead; Andrea Olland; Kristine Svenson; Eugene A. Terefenko; Ray Unwalla; James M. Wilhelm; Scott Wolfrom; Yuan Zhu; Zhiming Zhang; Puwen Zhang; Richard C. Winneker; Jay Wrobel

doi:10.1021/jm050358b

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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Fensome et al. (2005) studied this question.

synapsesocial.com/papers/6a75e77ef0e270a4f3b1da8f https://doi.org/10.1021/jm050358b

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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

Abstract

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Cite This Study

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

Abstract

Discussion

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