title: Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors.
abstract: 1-Aroylindoline, 1-aroyl-1,2,3,4-tetrahydroquinoline, and 1-aroylindole derivatives were synthesized and evaluated for anticancer activity. The 4-amino and 4-hydroxy-1-aroylindoles 26 and 27 with IC 50 of 0.9 and 0.6 microM, respectively, exhibited antitubulin activity superior or comparable to that of colchicine and combretastatin A-4. They also showed antiproliferative activity with IC 50 of 0.3-5.4 nM in a set of human cancer cell lines.
authors.affiliation: College of Pharmacy, Taipei Medical University, Taipei 110, Taiwan, Republic of China.
authors.forename: Jing-Ping
authors.initials: JP
authors.lastname: Liou
authors.forename: Zi-Yi
authors.initials: ZY
authors.lastname: Wu
authors.forename: Ching-Chuan
authors.initials: CC
authors.lastname: Kuo
authors.forename: Chi-Yen
authors.initials: CY
authors.lastname: Chang
authors.forename: Pei-Yi
authors.initials: PY
authors.lastname: Lu
authors.forename: Chi-Ming
authors.initials: CM
authors.lastname: Chen
authors.forename: Hsing-Pang
authors.initials: HP
authors.lastname: Hsieh
authors.forename: Jang-Yang
authors.initials: JY
authors.lastname: Chang
mesh_terms: D001704:Biopolymers / Q000737:chemistry*; D045744:Cell Line, Tumor; D006801:Humans; D007211:Indoles / Q000737:chemistry* / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D021241:Spectrometry, Mass, Electrospray Ionization; D014404:Tubulin / Q000737:chemistry / Q000187:drug effects*
chemical_list: D001704:Biopolymers; D007211:Indoles; D014404:Tubulin