A New Series of Estrogen Receptor Modulators : Effect of Alkyl Substituents on Receptor-Binding Affinity

概要

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New types of selective estrogen receptor modulators (SERMs) were synthesized and evaluated for their binding affinity and biological effect on reproductive cells. A proposed Head structure (B) was derivatized to provide compounds 30 and 44, which showed good estrogen-receptor bindSing affinity (K_i values: 6.3 and 10 nM, respectively), as well as minimal impact on mammary and uterine carcinoma cells. Introduction of an alkyl group in the core structure considerably enhanced receptor-binding affinity of the compounds tested. Synthesis and structure-activity relationships of these compounds are described.
公益社団法人日本薬学会の論文
2004-01-01