2. Academic Validation
  3. Synthesis and progesterone receptor antagonist activities of 6-aryl benzimidazolones and benzothiazolones

Synthesis and progesterone receptor antagonist activities of 6-aryl benzimidazolones and benzothiazolones

  • Bioorg Med Chem Lett. 2001 Oct 22;11(20):2747-50. doi: 10.1016/s0960-894x(01)00554-6.
P Zhang 1,  E A Terefenko,  J Wrobel,  Z Zhang,  Y Zhu,  J Cohen,  K B Marschke,  D Mais
Affiliations

Affiliation

  • 1 Medicinal Chemistry I, Chemical Sciences, Wyeth-Ayerst Research, Radnor, PA 19087, USA. zhang@war.wyeth.com
PMID: 11591515 DOI: 10.1016/s0960-894x(01)00554-6
Abstract

Novel 6-aryl benzimidazolones and benzothiazolones were prepared and examined as bioisosteres of the recently reported 6-aryl dihydroquinolines (1) for Progesterone Receptor (PR) antagonist activities. PR antagonist activities increased when compounds 9c-f possessed a more lipophilic group at position-1 and pendent aryl moiety para to NH moiety. Furthermore, conversion of carbonyl moiety of 9e,f to the thio-carbonyl led to benzoimidazolethiones 15a,b with significantly improved potency and binding affinity.

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