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Synthesis and Estrogen Receptor Affinity of 2,3‐Diarylindoles
Author(s) -
Strohmeier Josef,
Angerer Erwin Von
Publication year - 1987
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.19873200506
Subject(s) - chemistry , estrogen receptor , estrogen , dmba , in vivo , receptor , in vitro , stereochemistry , biochemistry , medicine , endocrinology , biology , cancer , breast cancer , carcinogenesis , microbiology and biotechnology , gene
2‐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.