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

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-…

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–…

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

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

Flavones and related compounds: synthesis and biological activity

D Leonte, D Ungureanu, V Zaharia - Molecules, 2023 - mdpi.com
… 3-kinase (PI3K) and phospho-protein kinase B (AKT) signaling … of the hydroxyl groups
of chrysin and kaempferol with … The natural flavones used as precursors were baicalein, …

Machine learning models for the classification of CK2 natural products inhibitors with molecular fingerprint descriptors

Y Liu, M Bi, X Zhang, N Zhang, G Sun, Y Zhou, L Zhao… - Processes, 2021 - mdpi.com
their inhibitory activity against CK2 with machine learning methods. In this study, classification
studies were conducted on 115 natural products as CK2 … vaccinia and promotes rapid cell-…

Discussion on the structural modification and anti-tumor activity of flavonoids

ZG Zhou, DD Li, Y Chen, X Chen… - Current Topics in …, 2022 - ingentaconnect.com
increase new biological activity functions. The synthesis route of … In addition, protein kinase
inhibitors exhibit more significant … Chrysin induces death of prostate cancer cells by inducing …

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

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-…