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

Эта публикация цитируется в 2 статьях

Communications

Phosphorylated flavonoids as selective carboxylesterase inhibitors

V. V. Abzianidze^a, D. S. Prokofieva^b, P. P. Beltyukov^a, V. A. Kuznetsov^a, A. S. Bogachenkov^c, K. S. Rodygin^c

^a Research Institute of Hygiene, Occupational Pathology and Human Ecology, Leningrad region, Russian Federation
^b Institute of Experimental Pharmacology, Leningrad Region, Russian Federation
^c Institute of Chemistry, St. Petersburg State University, St. Petersburg, Russian Federation

Аннотация: 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 k_i=2.0×10⁶ and 5.7×10⁶dm³mol⁻¹min⁻¹, respectively.

Язык публикации: английский

DOI: 10.1016/j.mencom.2019.01.020

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