7-Aroyl-aminoindoline-1-sulfonamides as a novel class of potent antitubulin agents.
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.
Chang
Jang-Yang
JY
Institute of Cancer Research, National Health Research Institutes, Taipei, Taiwan, Republic of China.
Hsieh
Hsing-Pang
HP
Chang
Chi-Yen
CY
Hsu
Kuo-Shun
KS
Chiang
Yi-Fang
YF
Chen
Chi-Ming
CM
Kuo
Ching-Chuan
CC
Liou
Jing-Ping
JP
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
D001704:Biopolymers; D007211:Indoles; D013449:Sulfonamides; D014404:Tubulin; D050257:Tubulin Modulators; D003078:Colchicine