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5-芳基茚满酮及其衍生物作为非甾体孕激素受体调节剂。

5-Aryl indanones and derivatives as non-steroidal progesterone receptor modulators.

机构信息

Chemical Sciences, Wyeth Research, Collegeville, PA 19426, USA.

出版信息

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6666-9. doi: 10.1016/j.bmcl.2009.10.008. Epub 2009 Oct 7.

DOI:10.1016/j.bmcl.2009.10.008
PMID:19864132
Abstract

Novel 5-aryl indanones, inden-1-one oximes, and inden-1-ols were synthesized and evaluated as progesterone receptor (PR) modulators using the T47D cell alkaline phosphatase assay. Both PR agonists and antagonists were achieved with appropriate 3- and 5-substitution from indanones and inden-1-ols while inden-1-one oximes provided only PR antagonists. Several compounds such as 10 and 11 demonstrated potent in vitro PR agonist potency similar to that of steroidal progesterone (1). In addition, a number of compounds (e.g., 12, 13, 17, 18) showed potent PR antagonist activity indicating the indanones and derivatives are promising PR modulator templates.

摘要

新型 5-芳基茚满酮、茚满-1-酮肟和茚满-1-醇被合成，并通过 T47D 细胞碱性磷酸酶测定法评估为孕激素受体 (PR) 调节剂。通过适当的 3-和 5-取代，从茚满酮和茚满-1-醇中获得了 PR 激动剂和拮抗剂，而茚满-1-酮肟仅提供了 PR 拮抗剂。一些化合物，如 10 和 11，表现出与甾体孕激素 (1) 相似的强体外 PR 激动剂活性。此外，一些化合物（如 12、13、17、18）表现出强 PR 拮抗剂活性，表明茚满酮和衍生物是有前途的 PR 调节剂模板。

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