title: Synthesis and antileukemic activity of (+-)-20-deoxyaminocamptothecin analogues.
abstract: The camptothecin analogues (+-)-7-ethyl-10-methoxy-20-deoxyaminocamptothecin (2) and (+-)-7-ethyl-10-hydroxy-20-deoxyaminocamptothecin.HCl (3) were synthesized from indolizine compound 4 via Friedländer condensation to construct a pentacyclic ring system, and were tested in a P388 mouse antileukemia assay. Compounds 2 and 3 were more active and less toxic than (+)-camptothecin (1), and therefore had higher therapeutic ratios.
authors.forename: A
authors.initials: A
authors.lastname: Ejima
authors.forename: H
authors.initials: H
authors.lastname: Terasawa
authors.forename: M
authors.initials: M
authors.lastname: Sugimori
authors.forename: S
authors.initials: S
authors.lastname: Ohsuki
authors.forename: K
authors.initials: K
authors.lastname: Matsumoto
authors.forename: Y
authors.initials: Y
authors.lastname: Kawato
authors.forename: H
authors.initials: H
authors.lastname: Tagawa
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002166:Camptothecin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D007941:Leukemia P388 / Q000188:drug therapy; D051379:Mice
chemical_list: D000970:Antineoplastic Agents; C062135:7-ethyl-10-hydroxy-20-deoxyaminocamptothecin; C062134:7-ethyl-10-methoxy-20-deoxyaminocamptothecin; D002166:Camptothecin