期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 84, 期 -, 页码 264-277出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.07.034
关键词
Carborane; Progesterone receptor (PR); Hydrophobic pharmacophore; Scaffold
资金
- Ministry of Education, Science, Sports and Culture, Japan [25460146]
- Grants-in-Aid for Scientific Research [25460146, 22136013] Funding Source: KAKEN
The progesterone receptor (PR) plays important roles in multiple physiological processes, including female reproduction. Here, we report the synthesis of nonsteroidal PR antagonists containing a boron cluster as the hydrophobic core. We found that 1,7-diphenyl-meta-carborane was the preferred substructure among the three carborane isomers. Compound 39 was the most potent PR antagonist (IC50: 29 nM). Compound 41 also exhibited potent activity (IC50: 93 nM), and did not bind to androgen receptor, glucocorticoid receptor or mineralocorticoid receptor. These compounds may be useful for investigating potential clinical applications of PR modulators. (C) 2014 Elsevier Masson SAS. All rights reserved.
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