Synthesis and antitumor evaluation of nitrovinyl biphenyls: anticancer agents based on allocolchicines |
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Authors: | Jain Nishant Yada Divya Shaik Thokhir B Vasantha Galanki Reddy P Surendra Kalivendi Shasi V Sreedhar B |
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Affiliation: | Centre for Chemical Biology, Indian Institute of Chemical Technology (Council of Scientific and Industrial Research), Hyderabad, India. |
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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 IC50 values in the range of 0.05–7 μM , 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 G2/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 G2/M phase of the cell cycle as the mode of action. |
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Keywords: | colchicines antitumor agents nitrovinyl biphenyls cytotoxicity tubulin polymerization |
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