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  • Title: Synthesis, anti-cancer evaluation of benzenesulfonamide derivatives as potent tubulin-targeting agents.
    Author: Yang J, Yang S, Zhou S, Lu D, Ji L, Li Z, Yu S, Meng X.
    Journal: Eur J Med Chem; 2016 Oct 21; 122():488-496. PubMed ID: 27423028.
    Abstract:
    A series of benzenesulfonamide derivatives were synthesized and evaluated for their anti-proliferative activity and interaction with tubulin. These new derivatives showed significant activities against cellular proliferative and tubulin polymerization. Compound BA-3b proved to be the most potent compound with IC50 value ranging from 0.007 to 0.036 μM against seven cancer cell lines, and three drug-resistant cancer cell lines, which indicated a promising anti-cancer agent. The target tubulin was also verified by dynamic tubulin polymerization assay and tubulin intensity assay.
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