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An Efficient One-Pot Synthesis and Anticancer Activity of 4'-Substituted Flavonoids

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Abstract

A number of 4'-substituted (R = H, Me, Cl, F) flavone derivatives is synthesized from 2-hydroxyacetophenones using the modified Baker–Venkataraman reaction. Compound [3-(4-fluorobenzoyl)-5- hydroxy-4'-fluoroflavone] was synthesized for the first time with the yield of 12%. Antiproliferative assays indicate that the synthesized flavones with F substituent at the 4' position demonstrate higher activity than the other flavone derivatives, particularly against HeLa and MCF-7 with the IC50 9.5 and 2.7 μM, respectively.

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Correspondence to X. Wang.

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Wang, X., Liu, J. & Zhang, Y. An Efficient One-Pot Synthesis and Anticancer Activity of 4'-Substituted Flavonoids. Russ J Gen Chem 88, 1036–1041 (2018). https://doi.org/10.1134/S1070363218050328

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  • DOI: https://doi.org/10.1134/S1070363218050328

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