Abstract
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 17 beta-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-hydroxybenzolmethylestradiol 12 exhibited the highest antiestrogenic activity of 63%. It also elicited 34% of the uterotrophic activity of estradiol.
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