Synthesis and biological evaluation of 7-arylindoline-1-benzenesulfonamides as a novel class of potent anticancer agents

MedChemComm
2010.0

Abstract

A series of 7-arylindoline-1-benzenesulfonamides were prepared and evaluated for anticancer activity. 7-(40 -Cyanophenyl)indoline-1-benzenesulfonamide 15 exhibited substantial antiproliferative activity with IC50 values ranging from 17–32 nM against a variety of human cancer cell lines, including MDR resistant line. Compound 15 (IC50 ¼ 1.5 mM) also showed more potent inhibition of tubulin polymerization than 4a (combretastatin A-4, IC50 ¼ 2.0 mM) and displayed strong binding to the colchicine binding site of the tubulin.

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