Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


Synthesis, Anticancer Activity and Inhibition of Tubulin Polymerization of Bisindole Sulfonates

Author(s): Ahmed Kamal, Y. V.V. Srikanth, M. Naseer Ahmed Khan, Md. Ashraf, Thokhir Basha Shaik, Shasi V. Kalivendi.


A new series of bisindole based sulfonates (4a-t) have been synthesized and evaluated for their anticancer activity against various human cancer cell lines. Some of these compounds exhibited good inhibitory activity against most of the cell lines tested. Interestingly all the compounds from the bisindole sulfonate series exhibited selective inhibition against MCF-7 cell line. Further these compounds have also been tested for their inhibition of tubulin polymerization. The compounds 4a, 4l, 4n, 4r and 4t demonstrated a dose dependent tubulin inhibition with IC50 values of 2.3, 1.7, 8.1, 6.0 and 10 μM, respectively. Thus, results have demonstrated that antiproliferative activity of these compounds is related to their inhibition of tubulin polymerization.

Keywords: Anticancer activity, Indoles, Sulfonates, Tubulin polymerization, Bisindole Sulfonates, cyclin-dependent kinases (CDKs), antiangiogenic, heterocyclic ring system, indole, mitomycin, cytotoxicity, Micro mass, Column chromatography

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Article Details

Year: 2012
Page: [242 - 250]
Pages: 9
DOI: 10.2174/157018012799129774
Price: $58