title: Synthesis and structure-activity relationships of novel benzofuran farnesyltransferase inhibitors.
abstract: A series of benzofuran-based farnesyltransferase inhibitors have been designed and synthesized as antitumor agents. Among them, 11f showed the most potent enzyme inhibitory activity (IC(50)=1.1nM) and antitumor activity in human cancer xenografts in mice.
authors.affiliation: Kamakura Research Laboratories, Chugai Pharmaceutical Co. Ltd., 200-Kajiwara, Kamakura, Kanagawa 247-8530, Japan.
authors.forename: Kohsuke
authors.initials: K
authors.lastname: Asoh
authors.forename: Masami
authors.initials: M
authors.lastname: Kohchi
authors.forename: Ikumi
authors.initials: I
authors.lastname: Hyoudoh
authors.forename: Tatsuo
authors.initials: T
authors.lastname: Ohtsuka
authors.forename: Miyako
authors.initials: M
authors.lastname: Masubuchi
authors.forename: Kenichi
authors.initials: K
authors.lastname: Kawasaki
authors.forename: Hirosato
authors.initials: H
authors.lastname: Ebiike
authors.forename: Yasuhiko
authors.initials: Y
authors.lastname: Shiratori
authors.forename: Takaaki A
authors.initials: TA
authors.lastname: Fukami
authors.forename: Osamu
authors.initials: O
authors.lastname: Kondoh
authors.forename: Toshiyuki
authors.initials: T
authors.lastname: Tsukaguchi
authors.forename: Nobuya
authors.initials: N
authors.lastname: Ishii
authors.forename: Yuko
authors.initials: Y
authors.lastname: Aoki
authors.forename: Nobuo
authors.initials: N
authors.lastname: Shimma
authors.forename: Masahiro
authors.initials: M
authors.lastname: Sakaitani
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001572:Benzofurans / Q000138:chemical synthesis* / Q000494:pharmacology; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D018360:Crystallography, X-Ray; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D051231:Farnesyltranstransferase / Q000037:antagonists & inhibitors* / Q000737:chemistry; D006801:Humans; D020128:Inhibitory Concentration 50; D051379:Mice; D009368:Neoplasm Transplantation; D015363:Quinolones / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D001572:Benzofurans; D004791:Enzyme Inhibitors; D015363:Quinolones; D051231:Farnesyltranstransferase; C105430:benzofuran; C402769:tipifarnib