The halogenation of natural flavonoids, baicalein and chrysin, enhances their affinity to human protein kinase CK2

E Marzec, M Świtalska, M Winiewska‐Szajewska… - IUBMB …, 2020 - Wiley Online Library
… ligand affinity to the catalytic subunit of human protein kinase CK2. Obtained results revealed
that substitution of baicalein and chrysin with halogen atom increases their binding affinity

Halogenated baicalein as a promising antiviral agent toward SARS-CoV-2 main protease

K Hengphasatporn, P Wilasluck… - Journal of Chemical …, 2022 - ACS Publications
… 3 μM) by blocking the human protein kinase CK2. (19) Typically, … to identify potential
halogenated flavonoids that can inhibit … ring enhanced the binding interaction with the protein

Synthesis of Novel Halogenated Heterocycles Based on o-Phenylenediamine and Their Interactions with the Catalytic Subunit of Protein Kinase CK2

M Winiewska-Szajewska, AM Maciejewska, E Speina… - Molecules, 2021 - mdpi.com
… between hydrophobicity and binding affinity, however, … protein–ligand complexes indicates
that any increase in ligand hydrophobicity is clearly reflected by an increase in binding affinity

Chrysin: Perspectives on contemporary status and future possibilities as pro-health agent

M Stompor-Gorący, A Bajek-Bil, M Machaczka - Nutrients, 2021 - mdpi.com
… responsible for the synthesis of chrysin and its derivatives, such as baicalin and wogonin, in
… of chrysin with chlorine increases the binding affinity to human protein kinase hCK2α, which …

Strategies of targeting CK2 in drug discovery: challenges, opportunities, and emerging prospects

Y Chen, Y Wang, J Wang, Z Zhou, S Cao… - Journal of Medicinal …, 2023 - ACS Publications
… , as a prodrug enhances its membrane permeability and … effects on CK2, while chrysin (75),
morin (76), baicalein (77), and … Unique activation mechanism of protein kinase CK2. The N-…

A promiscuous halogenase for the derivatization of flavonoids

D Kolling, M Stierhof, C Lasch, M Myronovskyi… - Molecules, 2021 - mdpi.com
… the tumour-associated human protein kinase CK2 have been … was previously reported
to increase their biological activity, it … Comparison to the predicted 13 C shift data of 6,8-Cl-chrysin

An overview of synthetic and semisynthetic flavonoid derivatives and analogues: perspectives in drug discovery

V Uivarosi, AC Munteanu, GM Nițulescu - Studies in Natural Products …, 2019 - Elsevier
Baicalein and quercetin are potently active against human … , 11 new chrysin derivatives
were synthesized to increase antiviral … protein kinases (MAPKs), phosphatidylinositol 3-kinase–…

Modification of flavonoids: Methods and influences on biological activities

C Li, T Dai, J Chen, M Chen, R Liang… - Critical Reviews in …, 2023 - Taylor & Francis
… of the observed increases or decreases in flavonoid activity … derivatives exhibited stronger
antimicrobial activity than baicalin … Hesperetin, luteolin, and chrysin were hydroxylated at the 8 …

Structural investigation of interactions between halogenated flavonoids and the lipid membrane along with their role as cytotoxic agents

A Dudek, N Szulc, A Pawlak, P Strugała-Danak… - Scientific Reports, 2024 - nature.com
… for tumour-associated human kinase CK2 and the observed … under the effect of flavonoids,
we have observed both an increase and a … The substitution of a bromine atom for baicalin (8-…

[PDF][PDF] Chrysin: perspectives on contemporary status and future possibilities as pro-health agent. Nutrients 2021; 13: 2038

M Stompor-Gorący, A Bajek-Bil, M Machaczka - 2021 - researchgate.net
… knowledge about natural sources of chrysin, its pharmacological activity … halogenation of
natural flavonoids, baicalein and chrysin, enhances their affinity to human protein kinase CK2