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
Journal of Medicinal Chemistry2005Vol. 48(16), pp. 5092–5095
Citations Over TimeTop 10% of 2005 papers
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
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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