Structure-activity relationships in the acronycine series.
Acronycine is active against a broad spectrum of solid tumors. Structure activity relationships demonstrated the crucial role of the 1,2-double bond. A hypothesis of bioactivation into 1,2-epoxide led to the development of a series of 1,2-dihydroxy-1,2-dihydroacronycine and 1,2-dihydroxy-1,2-dihydrobenzo[b]acronycine diesters that exhibited an increased potency when compared with the parent compound.
Michel
Sylvie
S
Laboratoire de Pharmacognosie de l'Université René Descartes, U.M.R. / C.N.R.S. Faculté des Sciences Pharmaceutiques et Biologiques, 4, Avenue de l'Observatoire, Paris, F-75006, France.
Seguin
Elisabeth
E
Tillequin
Fraņois
F
D000175:Acronine / Q000031:analogs & derivatives* / Q000494:pharmacology*; D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D000175:Acronine