title: 3-(3-Phenoxybenzyl)amino-β-carboline: a novel antitumor drug targeting α-tubulin.
abstract: 3-(3-Phenoxybenzyl)amino-β-carboline 2h showed extremely-high activity; the IC(50) value was 0.074 μM. To verify 2h-induced cell death types, we observed the chromatin condensation, the DNA fragmentation and activated caspase-3 using Hoechst 33342, agarose electrophoresis and western blot, and suggesting 2h-induced cell death type was apoptosis. Flow cytometry showed that 2h-treated cell was induced SubG1 cell population after G2/M cell cycle arrest. In addition, using affinity chromatography and peptide mass fingerprinting, we found that interacting protein with this compound was α-tubulin protein.
authors.affiliation: Department of Pure and Applied Chemistry, Faculty of Science and Technology, Tokyo University of Science (RIKADAI), Noda, Chiba 278-8510, Japan.
authors.forename: Reiko
authors.initials: R
authors.lastname: Ikeda
authors.forename: Masaki
authors.initials: M
authors.lastname: Kurosawa
authors.forename: Takazumi
authors.initials: T
authors.lastname: Okabayashi
authors.forename: Ayako
authors.initials: A
authors.lastname: Takei
authors.forename: Masamichi
authors.initials: M
authors.lastname: Yoshiwara
authors.forename: Tadashi
authors.initials: T
authors.lastname: Kumakura
authors.forename: Norio
authors.initials: N
authors.lastname: Sakai
authors.forename: Osamu
authors.initials: O
authors.lastname: Funatsu
authors.forename: Akinori
authors.initials: A
authors.lastname: Morita
authors.forename: Masahiko
authors.initials: M
authors.lastname: Ikekita
authors.forename: Yumi
authors.initials: Y
authors.lastname: Nakaike
authors.forename: Takeo
authors.initials: T
authors.lastname: Konakahara
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D016923:Cell Death / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells; D006801:Humans; D015394:Molecular Structure; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014404:Tubulin / Q000737:chemistry / Q000378:metabolism*
chemical_list: D000970:Antineoplastic Agents; D014404:Tubulin