Cytotoxic steroids with antiestrogenic activity of the 11alpha-acyloxyestra-1,3,5 (10) -triene series
Golubovskaia, L.E.; Smirnova, Z.S.; Tolkachev, V.N.; Rzheznikov, V.M.
Bioorganicheskaia Khimiia 32(2): 221-223
2006
ISSN/ISBN: 0132-3423 PMID: 16637294 Document Number: 596709
Esterification of 3-hydroxyl group in 11-acyloxyestra-1,3,5(10)-trienes with p-[bis(2-chloroethyl)amino]phenylacetic 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 for the 11alpha-hydroxylation of estra-1,3,5(10)-trienes.
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