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  • Title: Synthesis and structure-activity relationship of 4-azaheterocycle benzenesulfonamide derivatives as new microtubule-targeting agents.
    Author: Yang J, Zhou S, Ji L, Zhang C, Yu S, Li Z, Meng X.
    Journal: Bioorg Med Chem Lett; 2014 Nov 01; 24(21):5055-8. PubMed ID: 25278233.
    Abstract:
    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.
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