title: Antitumor agents. V. Synthesis and antileukemic activity of E-ring-modified (RS)-camptothecin analogues.
abstract: Several E-ring-modified analogues of (RS)-camptothecin were synthesized by total synthesis via Friedländer condensation and evaluated for cytotoxicity and antitumor activity against P388 mouse leukemia cells. Among them, (RS)-20-deoxyamino-7-ethyl-10-methoxycamptothecin (25c) was found to be more active than (RS)-camptothecin (1) in the in vivo assay.
authors.affiliation: Exploratory Research Laboratories I, Daiichi Pharmaceutical Co., Ltd., Tokyo, Japan.
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: M
authors.initials: M
authors.lastname: Yasuoka
authors.forename: H
authors.initials: H
authors.lastname: Tagawa
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002166:Camptothecin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D007941:Leukemia P388 / Q000188:drug therapy*; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; C062134:7-ethyl-10-methoxy-20-deoxyaminocamptothecin; D002166:Camptothecin