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

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...

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Bibliographic Details
Published in:Russian journal of bioorganic chemistry 2006-03, Vol.32 (2), p.201-203
Main Authors: Golubovskaya, L. E., Smirnova, Z. S., Tolkachev, V. N., Rzheznikov, V. M.
Format: Article
Language:English
Subjects:
Acetic acid
Cytotoxicity
Esterification
Hydroxyl groups
Hydroxylation
Steroids
Trienes
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Summary: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.
ISSN:1068-1620
1573-9163
1608-330X
DOI:10.1134/S1068162006020130