Canadian Journal of Chemistry

Design, chemical synthesis, and in vitro biological evaluation of simplified estradiol-adenosine hybrids as inhibitors of 17β-hydroxysteroid dehydrogenase type 1

M Berube, D Poirier

文献索引：Berube, Marie; Poirier, Donald Canadian Journal of Chemistry, 2009 , vol. 87, # 8 p. 1180 - 1199

全文：HTML全文

被引用次数: 16

摘要

A series of estradiol (E2) derivatives were designed to interact with both the substrate-and the cofactor-binding sites of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1). These analogues of potent E2-adenosine hybrid inhibitor EM-1745, where the adenosine moiety was replaced by a more stable benzene derivative, were synthesized from estrone using alkene cross-metathesis and Sonogashira coupling reactions as key steps. In vitro ...