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Phosphorylated flavonoids as selective carboxylesterase inhibitors

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A series of phosphorylated flavonoids has been synthesized and evaluated in vitro for inhibitory activity against carboxylesterase, acetylcholinesterase and butyrylcholinesterase as well as for their cytotoxicity towards human adenocarcinoma A549… Click to show full abstract

A series of phosphorylated flavonoids has been synthesized and evaluated in vitro for inhibitory activity against carboxylesterase, acetylcholinesterase and butyrylcholinesterase as well as for their cytotoxicity towards human adenocarcinoma A549 and human glioblastoma U251 cell lines. Diethylphosphoryl derivatives of chrysin and 7-hydroxyflavone were found to be the most effective with bimolecular rate constants for carboxylesterase inhibition ki = 2.0 × 106 and 5.7 × 106 dm3 mol−1 min−1, respectively.

Keywords: flavonoids selective; phosphorylated flavonoids; selective carboxylesterase; carboxylesterase; carboxylesterase inhibitors

Journal Title: Mendeleev Communications
Year Published: 2019

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