2. Academic Validation
  3. Novel pyrrole-containing progesterone receptor modulators

Novel pyrrole-containing progesterone receptor modulators

  • Bioorg Med Chem Lett. 2004 May 3;14(9):2185-9. doi: 10.1016/j.bmcl.2004.02.054.
Mark A Collins 1,  Valerie Hudak,  Reinhold Bender,  Andrew Fensome,  Puwen Zhang,  Lori Miller,  Richard C Winneker,  Zhiming Zhang,  Yuan Zhu,  Jeffrey Cohen,  Rayomond J Unwalla,  Jay Wrobel
Affiliations

Affiliation

  • 1 Chemical and Screening Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA.
PMID: 15081005 DOI: 10.1016/j.bmcl.2004.02.054
Abstract

A series of 1,4-dihydro-2H-[d][3,1]-benzoxazin-2-one and 1,3-dihydro-[3H]-indol-2-one containing 6- or 5-, respectively, appended substituted pyrrole moieties were synthesized and evaluated for their ability to modulate the activity of the Progesterone Receptor (PR). Key structural changes to the pyrrole moieties of these molecules were shown to have a predictive influence as to whether the compounds behaved as PR agonists or antagonists. Compounds with the 5(')-cyano-2(')-pyrrole moiety (e.g., 32, 33, and 38) were shown to be potent PR agonists (EC(50)'s of 1.1, 1.8, and 2.8 nM, respectively). Compounds with the 5(')-nitro-2(')-pyrrole moiety (e.g., 34 and 36) were shown to be PR antagonists (IC(50)'s of 180 and 36 nM, respectively).

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