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Synthesis, Uterotrophic, and Antiuterotrophic Activities of Some Estradiol Derivatives Containing Thiadiazole, Thiazoline, and Thiazolidinone Moieties
Author(s) -
ElTombary Alaa A.
Publication year - 1997
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.19973300906
Subject(s) - chemistry , thiazoline , biological activity , stereochemistry , aryl , chemical synthesis , organic chemistry , in vitro , biochemistry , alkyl
The effect of structural modification on the biological activity of hormones has been studied on five novel series of estradiol analogs bearing a variety of substituents at the 2‐position of the steroidal nucleus. The synthesized compounds include 2‐[2‐(5‐substituted amino‐1,3,4‐thiadiazol‐2‐yl)vinyl]estradiol 17ß‐acetate 5–9 , 2‐aroylmethylestradiols 10–12 , 2‐[2‐aryl‐2‐(substituted thiocarbamoylhydrazono)ethyl]estradiols 13–18 and their cyclic thiazoline 19–24 , and thiazolidinone derivatives 25–30 . Among the products, the p ‐hydroxybenzoylmethylestradiol 12 exhibited the highest antiestrogenic activity of 63%. It also elicited 34% of the uterotrophic activity of estradiol.