A series of 7-arylindoline-1-benzenesulfonamides were prepared and evaluated for anticancer activity. 7-(4′-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 = 1.5 μM) also showed more potent inhibition of tubulin polymerization than 4a (combretastatin A-4, IC50 = 2.0 μM) and displayed strong binding to the colchicine binding site of the tubulin.
ASJC Scopus subject areas
- Pharmaceutical Science
Chang, J-Y., Lai, M-J., Chang, Y-T., Lee, H. Y., Cheng, Y-C., Kuo, C-C., Su, M-C., Chang, C-Y., & Liou, J. P. (2010). Synthesis and biological evaluation of 7-arylindoline-1-benzenesulfonamides as a novel class of potent anticancer agents. MedChemComm, 1(2), 152-155. https://doi.org/10.1039/c0md00052c