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  • Title: Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors.
    Author: Liou JP, Wu ZY, Kuo CC, Chang CY, Lu PY, Chen CM, Hsieh HP, Chang JY.
    Journal: J Med Chem; 2008 Jul 24; 51(14):4351-5. PubMed ID: 18588280.
    Abstract:
    1-Aroylindoline, 1-aroyl-1,2,3,4-tetrahydroquinoline, and 1-aroylindole derivatives were synthesized and evaluated for anticancer activity. The 4-amino and 4-hydroxy-1-aroylindoles 26 and 27 with IC 50 of 0.9 and 0.6 microM, respectively, exhibited antitubulin activity superior or comparable to that of colchicine and combretastatin A-4. They also showed antiproliferative activity with IC 50 of 0.3-5.4 nM in a set of human cancer cell lines.
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