Antitumor activity of pyridocarbazole and benzopyridoindole derivatives that inhibit protein kinase CK2

R Prudent, V Moucadel, CH Nguyen, C Barette… - Cancer research, 2010 - AACR
The alkyloid compound ellipticine derived from the berrywood tree is a topoisomerase II
poison that is used in ovarian and breast cancer treatment. In this study, we report the …

Study on the anticancer activity of coumarin derivatives by molecular modeling

XY Huang, ZJ Shan, HL Zhai, L Su… - Chemical Biology & …, 2011 - Wiley Online Library
Protein kinase 2 (CK2) is a potential target, and the coumarins were identified as the
attractive CK2 inhibitors. In this study, two models (CoMFA and CoMSIA) were established …

A note of caution on the role of halogen bonds for protein kinase/inhibitor recognition suggested by high-and low-salt CK2α complex structures

B Guerra, N Bischoff, VG Bdzhola… - ACS Chemical …, 2015 - ACS Publications
CK2 is a Ser/Thr kinase recruited by tumor cells to avoid cell death. 4′-Carboxy-6, 8-
dibromo-flavonol (FLC26) is a nanomolar CK2 inhibitor reducing the physiological …

[HTML][HTML] Synthesis of Novel Acyl Derivatives of 3-(4,5,6,7-Tetrabromo-1H-benzimidazol-1-yl)propan-1-ols—Intracellular TBBi-Based CK2 Inhibitors with Proapoptotic …

K Chojnacki, P Wińska, O Karatsai… - International Journal of …, 2021 - mdpi.com
Protein kinase CK2 has been considered as an attractive drug target for anti-cancer therapy.
The synthesis of N-hydroxypropyl TBBi and 2MeTBBi derivatives as well as their respective …

Design and synthesis of CK2 inhibitors

M Makowska, E Łukowska-Chojnacka… - Molecular and cellular …, 2011 - Springer
A series of new polybrominated benzimidazoles and benzotriazoles has been synthesized
and their influence on the activity of protein kinase CK2 was evaluated. It was revealed that …

Synthesis and SAR of inhibitors of protein kinase CK2: novel tricyclic quinoline analogs

M Haddach, F Pierre, CF Regan, C Borsan… - Bioorganic & medicinal …, 2012 - Elsevier
Protein kinase CK2 is a potential drug target for many diseases including cancer and
inflammation disorders. The crystal structure of clinical candidate CX-4945 1 with CK2 …

Biological properties and structural study of new aminoalkyl derivatives of benzimidazole and benzotriazole, dual inhibitors of CK2 and PIM1 kinases

K Chojnacki, P Wińska, M Wielechowska… - Bioorganic …, 2018 - Elsevier
The new aminoalkyl-substituted derivatives of known CK2 inhibitors 4, 5, 6, 7-tetrabromo-1H-
benzimidazole (TBBi) and 4, 5, 6, 7-tetrabromo-1H-benzotriazole (TBBt) were synthesized …

[HTML][HTML] Exploring the Pivotal Role of the CK2 Hinge Region Sub-Pocket in Binding with Tricyclic Quinolone Analogues by Computational Analysis

Y Zhou, N Zhang, S Tang, X Qi, L Zhao, R Zhong… - Molecules, 2017 - mdpi.com
Protein kinase CK2 has been considered as an attractive therapeutic target of cancer
therapy. The tricyclic quinoline compound CX-4945 is the first representative of CK2 …

Dihydrobenzo[4,5]imidazo[1,2-a]pyrimidine-4-ones as a new class of CK2 inhibitors

MV Protopopov, OV Ostrynska, SA Starosyla… - Molecular Diversity, 2018 - Springer
Identification of new small molecules inhibiting protein kinase CK2 is highly required for the
study of this protein's functions in cell and for the further development of novel …

Discovery and SAR of 5-(3-Chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic Acid (CX-4945), the First Clinical Stage Inhibitor of Protein Kinase CK2 for the …

F Pierre, PC Chua, SE O'Brien… - Journal of medicinal …, 2011 - ACS Publications
Herein we chronicle the discovery of CX-4945 (25n), a first-in-class, orally bioavailable ATP-
competitive inhibitor of protein kinase CK2 in clinical trials for cancer. CK2 has long been …