1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists
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- 作者：Jeffrey C. Kern ; Eugene Terefenko ; Eugene Trybulski ; Thomas J. Berrodin ; Jeffrey Cohen ; Richard C. Winneker ; Matthew R. Yudt ; Zhiming Zhang ; Yuan Zhu ; Puwen Zhang
- 关键词：Progesterone ; Antagonist ; Modulator ; Tetrahydronaphthalene ; Nuclear hormone ; 1-Methyl-1H-pyrrole-2-carbonitrile
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2010
- 出版时间：15 August 2010
- 年：2010
- 卷：20
- 期：16
- 页码：4816-4818
- 全文大小：466 K
文摘
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.