Antileukemic compounds derived by chemical modification of macrocyclic trichothecenes. 2. Derivatives of roridins A and H and verrucarins A and J.
Various 8 beta-hydroxy, 16-hydroxy, and 9 beta,10 beta-epoxy derivatives of roridins A and H and verrucarins A and J have been prepared and tested in vivo against P388 mouse leukemia. The 9 beta,10 beta-epoxy derivatives and 16-hydroxy derivatives consistently exhibit very high activity. The 8 beta-hydroxy-9 beta,10 beta-epoxy and 16-hydroxy-9 beta,10 beta-epoxy derivatives of verrucarin A and roridin A exhibit extraordinary activity against P388. The 8 beta-hydroxy-9 beta,10 beta-epoxy and 16-hydroxy-9 beta,10 beta-epoxy derivatives of verrucarin A and roridin A exhibit extraordinary against P388.
D000818:Animals; D002460:Cell Line; D055598:Chemical Phenomena; D002621:Chemistry; D004852:Epoxy Compounds; D006900:Hydroxylation; D007942:Leukemia, Experimental / Q000188:drug therapy*; D051379:Mice; D012717:Sesquiterpenes / Q000138:chemical synthesis*; D013329:Structure-Activity Relationship; D014255:Trichothecenes / Q000138:chemical synthesis* / Q000627:therapeutic use
D004852:Epoxy Compounds; D012717:Sesquiterpenes; D014255:Trichothecenes; C040377:roridin H; C035445:verrucarin J; C005348:muconomycin A; C038849:roridin A