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1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists |
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| Authors: | Jeffrey C. Kern Eugene Terefenko Eugene Trybulski Thomas J. Berrodin Jeffrey Cohen Richard C. Winneker Matthew R. Yudt Zhiming Zhang Yuan Zhu Puwen Zhang |
| Affiliation: | 1. Chemical Sciences, Pfizer Global Research and Development, 500 Arcola Road, Collegeville, PA 19426, USA;2. Musculoskeletal Biology, Pfizer Global Research and Development, 500 Arcola Road, Collegeville, PA 19426, USA |
| 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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