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Design, Synthesis, and Anticancer Evaluation of Tetrazole-Fused Benzoxazole Derivatives as Tubulin Binding Agents

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Abstract

A novel series of tetrazole fused benzoxazole derivatives 9a9j are synthesized, and their structures are characterized by 1H and 13C NMR, and mass spectra. The compounds 9a, 9b, 9g, 9h, and 9j demonstrate the highest activity. The compounds 9b and 9g exhibit good anticancer activity, in particular against MCF7, Hop62, and A-549 cell lines with the range of GI50 values from <0.1 to 4.56 μM. Molecular docking study is carried out for the compounds 9a9j, according to which the compound 9b forms one hydrogen bond with THR766 with the highest docking score (–7.33). This indicates that 9b is effeciently binging to tubulin site.

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Correspondence to P. Ravikumar.

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Ravikumar, P., Raolji, G.S.B., Venkata Sastry, K. et al. Design, Synthesis, and Anticancer Evaluation of Tetrazole-Fused Benzoxazole Derivatives as Tubulin Binding Agents. Russ J Gen Chem 88, 2183–2189 (2018). https://doi.org/10.1134/S1070363218100250

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