Synthesis and structure-activity relationship of 4-azaheterocycle benzenesulfonamide derivatives as new microtubule-targeting agents.

A series of 1-sulfonyl indolines was synthesized and evaluated for antiproliferative activity. The most potent compounds 9 a and 9 e showed significant cytotoxicity (IC50 in the range of 0.055-0.105 and 0.039-0.112 μM, respectively) against four human cancer cell lines HCT116, PC3, HepG2 and SK-OV-3. The structure-activity relationship of this series of sulfonamides, including the influence of azaheterocycle rings, substituent at the different positions of indoline, and the cyclopropane moiety, was described.