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A new series of estrogen receptor modulators: effect of alkyl substituents on receptor-binding affinity. 2004
Atsushi Kamada, and
Atsushi Sasaki, and
Noritaka Kitazawa, and
Tadashi Okabe, and
Kazumasa Nara, and
Shinichi Hamaoka, and
Shin Araki, and
Hiroaki Hagiwara
Tsukuba Research Laboratories, Eisai Co., Ltd.
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 the core structure considerably enhanced receptor-binding affinity of the compounds tested. Synthesis and structure-activity relationships of these compounds are described.
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