2. Academic Validation
  3. Synthesis and identification of novel oxa-steroids as progesterone receptor antagonists

Synthesis and identification of novel oxa-steroids as progesterone receptor antagonists

  • Bioorg Med Chem Lett. 2007 Feb 15;17(4):907-10. doi: 10.1016/j.bmcl.2006.11.062.
Fu-An Kang 1,  George Allan,  Jihua Guan,  Nareshkumar Jain,  Olivia Linton,  Pamela Tannenbaum,  Jun Xu,  Peifang Zhu,  Joseph Gunnet,  Xin Chen,  Keith Demarest,  Scott Lundeen,  Zhihua Sui
Affiliations

Affiliation

  • 1 Johnson and Johnson Pharmaceutical Research and Development, LLC, 665 Stockton Drive, Exton, PA 19341, USA. fkang@prdus.jnj.com
PMID: 17169557 DOI: 10.1016/j.bmcl.2006.11.062
Abstract

A novel series of oxa-steroids 6 derived from (8S, 13S, 14R)-7-oxa-estra-4,9-diene-3,17-dione 1 have been synthesized and identified as potent and selective Progesterone Receptor antagonists. These novel oxa-steroids showed similar potency to mifepristone. Preliminary SAR study resulted in the most potent 17-phenylethynyl oxa-steroid 6i wih an IC(50) of 1.4nM. In contrast to the equipotent mifepristone toward the Progesterone Receptor (PR) and Glucocorticoid Receptor (GR), compound 6i had over 200-fold selectivity for PR over GR.

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