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 5.7×106dm3mol−1min−1, respectively.
Citation:
V. V. Abzianidze, D. S. Prokofieva, P. P. Beltyukov, V. A. Kuznetsov, A. S. Bogachenkov, K. S. Rodygin, “Phosphorylated flavonoids as selective carboxylesterase inhibitors”, Mendeleev Commun., 29:1 (2019), 61–63
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https://www.mathnet.ru/eng/mendc/v29/i1/p61
This publication is cited in the following 2 articles:
P. A. Volkov, K. O. Khrapova, A. A. Telezhkin, A. I. Albanov, B. A. Trofimov, “Three-component reaction between phenanthridine, acetylenic ketones and bis(polyfluoroalkyl) H-phosphonates: synthesis of E-N-acylethenyl-6-bis(polyfluoroalkyl)phosphoryl-5,6-dihydrophenanthridines”, Russ Chem Bull, 73:1 (2024), 221
Yan Jia, Jiayue Wang, Peng Li, Xiaochi Ma, Keli Han, “Directionally Modified Fluorophores for Super-Resolution Imaging of Target Enzymes: A Case Study with Carboxylesterases”, J. Med. Chem., 64:21 (2021), 16177