[Cytotoxic steroids with antiestrogenic activity of the 11alpha-acyloxyestra-1,3,5(10)-triene series].
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.
Golubovskaia
L E
LE
Smirnova
Z S
ZS
Tolkachev
V N
VN
Rzheznikov
V M
VM
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D004963:Estrenes / Q000138:chemical synthesis / Q000494:pharmacology*; D004965:Estrogen Antagonists / Q000138:chemical synthesis / Q000494:pharmacology*; D005260:Female; D006801:Humans; D008325:Mammary Neoplasms, Experimental / Q000188:drug therapy; D051379:Mice; D009376:Neoplasms, Hormone-Dependent; D010051:Ovarian Neoplasms
D000970:Antineoplastic Agents; D004963:Estrenes; D004965:Estrogen Antagonists