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Influence of Derivatisation of the Hydroxy Groups in 1,1‐Bis‐(4‐hydroxyphenyl)‐2‐phenylbut‐1‐ene on Estradiol Receptor Affinity and Mammary Tumor Inhibiting Properties
Author(s) -
Schuderer Michael L.,
Schneider Martin R.
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.19873200713
Subject(s) - chemistry , potency , ether , ene reaction , estrogen receptor , carbamate , stereochemistry , receptor , estrogen , in vitro , biochemistry , medicine , organic chemistry , endocrinology , biology , cancer , breast cancer
Abstract The phenolic hydroxy groups of 1,1‐bis‐(4‐hydroxyphenyl)‐2‐phenylbut‐1‐ene ( 1 ) were converted to esters of different chain length and degree of halogen substitution, and to carbamate, imidoester and ether derivatives. Most of the products maintain the affinity to the estrogen receptor. The acetate 2 has a better antitumor potency than 1 .