2. Academic Validation
  3. 1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists

1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists

  • Bioorg Med Chem Lett. 2010 Aug 15;20(16):4816-8. doi: 10.1016/j.bmcl.2010.06.109.
Jeffrey C Kern 1,  Eugene Terefenko,  Eugene Trybulski,  Thomas J Berrodin,  Jeffrey Cohen,  Richard C Winneker,  Matthew R Yudt,  Zhiming Zhang,  Yuan Zhu,  Puwen Zhang
Affiliations

Affiliation

  • 1 Chemical Sciences, Pfizer Global Research and Development, 500 Arcola Road, Collegeville, PA 19426, USA. Jkern75@hotmail.com
PMID: 20638844 DOI: 10.1016/j.bmcl.2010.06.109
Abstract

Non-steroidal 1-methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalenes and acyclic derivatives were evaluated as novel series of Progesterone Receptor (PR) antagonists using the T47D cell Alkaline Phosphatase assay. Moderate to potent PR antagonists were achieved with these scaffolds. Several compounds (e.g., 15 and 20) demonstrated low nanomolar PR antagonist potency and good selectivity versus Other steroid receptors.

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