title: 7-Aroyl-aminoindoline-1-sulfonamides as a novel class of potent antitubulin agents.
abstract: A novel series of 7-aroyl-aminoindoline-1-benzenesulfonamides showed excellent activity as inhibitors of tubulin polymerization through binding with the colchicine binding site of microtubules. Compound 15 and 16 display IC50 values of 1.1 and 1.2 microM, respectively. Compound 15 inhibited the human cancer cell growth of KB, MKN45, H460, HT29, and TSGH, as well as one human-resistant cancer line of KB-vin 10, with an IC50 of 9.6, 8.8, 9.4, 8.6, 10.8, and 8.9 nM, respectively.
authors.affiliation: Institute of Cancer Research, National Health Research Institutes, Taipei, Taiwan, Republic of China.
authors.forename: Jang-Yang
authors.initials: JY
authors.lastname: Chang
authors.forename: Hsing-Pang
authors.initials: HP
authors.lastname: Hsieh
authors.forename: Chi-Yen
authors.initials: CY
authors.lastname: Chang
authors.forename: Kuo-Shun
authors.initials: KS
authors.lastname: Hsu
authors.forename: Yi-Fang
authors.initials: YF
authors.lastname: Chiang
authors.forename: Chi-Ming
authors.initials: CM
authors.lastname: Chen
authors.forename: Ching-Chuan
authors.initials: CC
authors.lastname: Kuo
authors.forename: Jing-Ping
authors.initials: JP
authors.lastname: Liou
mesh_terms: D001665:Binding Sites; D001704:Biopolymers; D045744:Cell Line, Tumor; D003078:Colchicine / Q000378:metabolism / Q000494:pharmacology; D018432:Drug Resistance, Multiple; D019008:Drug Resistance, Neoplasm; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008870:Microtubules / Q000378:metabolism; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014404:Tubulin / Q000737:chemistry / Q000378:metabolism; D050257:Tubulin Modulators / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D001704:Biopolymers; D007211:Indoles; D013449:Sulfonamides; D014404:Tubulin; D050257:Tubulin Modulators; D003078:Colchicine