title: Structure-activity relationship of a novel antitumor ansamycin antibiotic trienomycin A and related compounds.
abstract: Various derivatives of trienomycin A (1) were prepared and tested for cytocidal activities. All the derivatives except for 22-O-methyltrienomycin A (5) showed reduced cytotoxicity compared with 1. It is concluded that the existence of a triene moiety, free 13-OH and an acyl group at C-11 owe important role for cytocidal activity.
authors.affiliation: Kitasato Institute, School of Pharmaceutical Sciences, Kitasato University, Tokyo, Japan.
authors.forename: S
authors.initials: S
authors.lastname: Funayama
authors.forename: Y
authors.initials: Y
authors.lastname: Anraku
authors.forename: A
authors.initials: A
authors.lastname: Mita
authors.forename: Z B
authors.initials: ZB
authors.lastname: Yang
authors.forename: K
authors.initials: K
authors.lastname: Shibata
authors.forename: K
authors.initials: K
authors.lastname: Komiyama
authors.forename: I
authors.initials: I
authors.lastname: Umezawa
authors.forename: S
authors.initials: S
authors.lastname: Omura
mesh_terms: D000409:Alanine / Q000031:analogs & derivatives; D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000138:chemical synthesis; D003509:Cyclohexanecarboxylic Acids / Q000138:chemical synthesis / Q000494:pharmacology; D005260:Female; D006367:HeLa Cells / Q000187:drug effects; D007941:Leukemia P388 / Q000188:drug therapy; D051379:Mice; D013329:Structure-Activity Relationship
chemical_list: D000903:Antibiotics, Antineoplastic; D003509:Cyclohexanecarboxylic Acids; C045958:trienomycin A; D000409:Alanine