Steroidal derivatives. Part 1: some novel steroidal thiosemicarbazones. Their synthesis, anticancer and endocrinological activities.
The synthesis of several novel thiosemicarbazone derivatives of steroids, including estrogens and androgens, is described. Evaluation of the products in P 388 Lymphocytic Leukemia indicated no anticancer activity. The endocrinological screening showed that estrogenicity is slightly reduced but not abolished in the thiosemicarbazones derived from estrone-3-methyl ether (compounds 1, 2 and 4). The androgenic activity of the thiosemicarbazones derived from testosterone (compounds 7--9) was more pronounced than that of testosterone. Among the same thiosemicarbazone derivatives 7--9, only o-tolyl derivative 8 exhibited anabolic activity.
D000818:Animals; D000970:Antineoplastic Agents; D004958:Estradiol / Q000494:pharmacology; D005260:Female; D008297:Male; D051379:Mice; D009132:Muscles / Q000187:drug effects; D009929:Organ Size / Q000187:drug effects; D011467:Prostate / Q000187:drug effects; D051381:Rats; D013256:Steroids / Q000138:chemical synthesis* / Q000494:pharmacology; D013739:Testosterone / Q000494:pharmacology; D013882:Thiosemicarbazones / Q000138:chemical synthesis* / Q000494:pharmacology; D014599:Uterus / Q000187:drug effects
D000970:Antineoplastic Agents; D013256:Steroids; D013882:Thiosemicarbazones; D013739:Testosterone; D004958:Estradiol