A new series of estrogen receptor modulators: Effect of alkyl substituents on receptor-binding affinity

A Kamada, A Sasaki, N Kitazawa, T Okabe…

文献索引：Kamada, Atsushi; Sasaki, Atsushi; Kitazawa, Noritaka; Okabe, Tadashi; Nara, Kazumasa; Hamaoka, Shinichi; Araki, Shin; Hagiwara, Hiroaki Chemical and Pharmaceutical Bulletin, 2004 , vol. 52, # 1 p. 79 - 88

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被引用次数: 11

摘要

New types of selective estrogen receptor modulators (SERMs) were synthesized and evaluated for their binding affinity and biological effect on reproductive cells. A proposed lead structure (B) was derivatized to provide compounds 30 and 44, which showed good estrogen-receptor binding 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 ...