2. Academic Validation
  3. 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

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

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

Affiliation

  • 1 Chemical and Screening Sciences, Women's Health Research Institute, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA. [email protected]
PMID: 16078826 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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