Steroidal alpha-methylene delta-lactones as potential antitumor agents.
Four novel steroidal alpha-methylene delta-lactones have been synthesized and shown to be active against human nasopharyngeal carcinoma (KB) cells in culture. The syntheses involved the use of known alpha-methylenation procedures. In addition, the lactone 6 was directly methylenated by reaction with CH2O/KOH or Et2NH/CH2O/Et2NH.HCl. The formation of a cysteine adduct (15) with the alpha-methylene lactone 10 is reported.
D000970:Antineoplastic Agents / Q000138:chemical synthesis*; D002455:Cell Division / Q000187:drug effects; D002478:Cells, Cultured; D006801:Humans; D007783:Lactones / Q000138:chemical synthesis* / Q000494:pharmacology; D009303:Nasopharyngeal Neoplasms; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D007783:Lactones