Synthesis and structure–activity relationships of analogs of EM-652 (acolbifene), a pure selective estrogen receptor modulator. Study of nitrogen substitution

…, C Ouellet, A Schwerdtfeger, Y Merand…

文献索引：Gauthier; Caron; Cloutier; Dory; Favre; Larouche; Mailhot; Ouellet; Schwerdtfeger; Leblanc; Martel; Simard; Merand; Belanger; Labrie Journal of Medicinal Chemistry, 1997 , vol. 40, # 14 p. 2117 - 2122

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被引用次数: 13

摘要

EM-652 (acolbifene) analogs have been synthesized as selective estrogen receptor modulators. Substitution on the nitrogen atom of these 2 H-1-benzopyran derivatives has been studied for its influence on antiestrogenic activity. Binding to the rat estrogen receptor, inhibition of estradiol-stimulated proliferation of T-47D breast cancer cells, as well as antiuterotrophic and uterotrophic activities in ovariectomized mice have been evaluated. 2 ...