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.
Abbreviations
- DDQ:
-
2,3-dichloro-5,6-dicyano-1,4-benzoquinone
- DMAP:
-
4-dimethylaminopyridine
- TEA:
-
triethylamine
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Original Russian Text © L.E. Golubovskaya, Z.S. Smirnova, V.N. Tolkachev, V.M. Rzheznikov, 2006, published in Bioorganicheskaya Khimiya, 2006, Vol. 32, No. 2, pp. 221–224.
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Golubovskaya, L.E., Smirnova, Z.S., Tolkachev, V.N. et al. Cytotoxic steroids with antiestrogenic activity of the 11α-acyloxyestra-1,3,5(10)-triene series. Russ J Bioorg Chem 32, 201–203 (2006). https://doi.org/10.1134/S1068162006020130
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DOI: https://doi.org/10.1134/S1068162006020130