Discovery of thiochroman and chroman derivatives as pure antiestrogens and their structure–activity relationship

…, T Tsunenari, K Taniguchi, I Ohizumi, S Kaiho…

文献索引：Kanbe, Yoshitake; Kim, Myung-Hwa; Nishimoto, Masahiro; Ohtake, Yoshihito; Kato, Nobuaki; Tsunenari, Toshiaki; Taniguchi, Kenji; Ohizumi, Iwao; Kaiho, Shin-ichi; Morikawa, Kazumi; Jo, Jae-Chon; Lim, Hyun-Suk; Kim, Hak-Yeop Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 14 p. 4803 - 4819

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被引用次数: 20

摘要

In order to develop pure antiestrogens, a series of 7-hydroxy-3-(4-hydroxyphenyl)-3- methylchroman and 7-hydroxy-3-(4-hydroxyphenyl)-3-methylthiochroman derivatives with sulfoxide containing side chains at the 4-position were designed, synthesized, and evaluated. Among them, compounds 14b and 24b functioned as pure antiestrogens with the ability to downregulate ER, and their in vitro and in vivo antiestrogen activities were similar ...