Synthesis and antitumor evaluation of nitrovinyl biphenyls: anticancer agents based on allocolchicines.
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Jain N, Yada D, Shaik TB, Vasantha G, Reddy PS, Kalivendi SV, Sreedhar B
Synthesis and antitumor evaluation of nitrovinyl biphenyls: anticancer agents based on allocolchicines.
ChemMedChem. 2011 May 2;6(5):859-68. doi: 10.1002/cmdc.201100019. Epub 2011 Apr 6.
- PubMed ID
- 21472861 [ View in PubMed]
- Abstract
A new class of nitrovinyl biphenyl compounds based on the structures of colchicines and allocolchicines were designed, synthesized, and shown to inhibit tubulin polymerization and cause mitotic arrest. A majority of these compounds were found to possess potent anticancer properties, with IC(50) values in the range of 0.05-7 muM, and are equally potent with colchicine in HeLa and MCF-7 cells. Compounds 14 e and 14 f inhibited tubulin assembly by more than 60 %, and flow cytometry studies indicated growth arrest of cells in the G(2)/M phase of the cell cycle in a concentration-dependent manner. Treatment of cells with 14 f resulted in upregulation of cyclin B1 and aurora kinase B mRNA levels, corresponding to growth arrest in the G(2)/M phase of the cell cycle as the mode of action.