Abstract
Abstract2‐Phenylindoles with aromatic substituents at C‐3 and hydroxy functions at the aromatic rings were synthesized and tested for their binding affinity for the calf uterine estrogen receptor. Most of these indoles bind to the estrogen receptor. The highest binding affinity (1,25 % of estradiol) was found with 3‐(4‐hydroxyphenyl)‐2‐phenylindole (3b). The acetate of 3b was studied in vivo. It was devoid of estrogenic or antiestrogenic activity in the mouse and inhibited only weakly the growth of hormone‐dependent DMBA‐induced rat mammary tumors.
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