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Issue 9, 2011
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2-Anilinonicotinyl linked 1,3,4-oxadiazole derivatives: Synthesis, antitumour activity and inhibition of tubulin polymerization

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Abstract

A series of 2-anilinonicotinyl linked 1,3,4-oxadiazoles was synthesized and evaluated for their antitumour activity against various cancer cell lines, inhibition of tubulin polymerization and cell cycle effects. Some of these compounds showed good antiproliferative activity with GI50 values ranging from 4.57 to 97.09 μM in the human cancer cell lines and one of the compounds 5m showed potent antitumour efficacy in all the cell lines tested. This compound also inhibited tubulin polymerization under both in vitro and in vivo conditions. Analysis of tubulin by Western blot experiments demonstrated that 5m depolymerizes microtubules by causing disturbances in the ratio of soluble versus polymerized tubulin in cells, leading to the cell cycle arrest at G2/M phase of the cell cycle followed by activation of caspase-3 activity and apoptotic cell death.

Graphical abstract: 2-Anilinonicotinyl linked 1,3,4-oxadiazole derivatives: Synthesis, antitumour activity and inhibition of tubulin polymerization

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Publication details

The article was received on 05 Oct 2010, accepted on 12 Feb 2011 and first published on 19 May 2011


Article type: Concise Article
DOI: 10.1039/C0MD00177E
Med. Chem. Commun., 2011,2, 819-823

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    2-Anilinonicotinyl linked 1,3,4-oxadiazole derivatives: Synthesis, antitumour activity and inhibition of tubulin polymerization

    A. Kamal, Y. V. V. Srikanth, T. B. Shaik, M. N. A. Khan, Md. Ashraf, M. K. Reddy, K. A. Kumar and S. V. Kalivendi, Med. Chem. Commun., 2011, 2, 819
    DOI: 10.1039/C0MD00177E

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