Cytotoxic steroids with antiestrogenic activity of the 11α-acyloxyestra-1,3,5(10)-triene series


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Abstract

Esterification of 3-hydroxyl group in 11α-acyloxyestra-1,3,5(10)-trienes with p-[bis(2-chloroethyl)amino]phenyl acetic acid led to antitumor steroids displaying antiestrogenic and cytotoxic activities. Our substances exhibit their activities on the model of murine mammary adenocarcinoma Ca-755, with inhibition of the tumor growth being 94-99%. A new approach was used to the 11α-hydroxylation of estra-1,3,5(10)-trienes.

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