含四氢萘衍生物的 1-甲基-1H-吡咯-2-甲腈作为非甾体孕激素受体拮抗剂。
1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists.
机构信息
Chemical Sciences, Pfizer Global Research and Development, 500 Arcola Road, Collegeville, PA 19426, USA.
出版信息
Bioorg Med Chem Lett. 2010 Aug 15;20(16):4816-8. doi: 10.1016/j.bmcl.2010.06.109. Epub 2010 Jun 25.
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.
含四氢萘和非环衍生物的非甾体 1-甲基-1H-吡咯-2-甲腈被评估为孕激素受体 (PR) 拮抗剂的新型系列，使用 T47D 细胞碱性磷酸酶测定法。这些支架实现了中度至强效的 PR 拮抗剂。几种化合物（例如 15 和 20）表现出低纳摩尔 PR 拮抗剂活性和对其他甾体受体的良好选择性。
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