Synthesis, biological properties and structural study of new halogenated azolo[4,5-b]pyridines as inhibitors of CK2 kinase

K Chojnacki*, Christine Toelzer, et al.

*Corresponding author for this work

Research output: Contribution to journalArticle (Academic Journal)peer-review


The new halogenated 1H-triazolo[4,5-b]pyridines and 1H-imidazo[4,5-b]pyridines were synthesised as analogues of known CK2 inhibitors: 4,5,6,7-tetrabromo-1H-benzotriazole (TBBt) and 4,5,6,7-tetrabromo-1H-benzimidazole (TBBi). Their influence on the activity of recombinant human CK2α, CK2α’ and PIM1 kinases was determined. The most active inhibitors were di- and trihalogenated 1H-triazolo[4,5-b]pyridines (4a, 5a and 10a) with IC50 values 2.56, 3.82 and 3.26 μM respectively for CK2α. Furthermore, effect on viability of cancer cell lines MCF-7 (human breast adenocarcinoma) and CCRF-CEM (T lymphoblast leukemia) of all final compounds was evaluated. Finally, three crystal structures of complexes of CK2α1-335 with inhibitors 4a, 5a and 10a were obtained. In addition, new protocol was used to obtain high-resolution crystal structures of CK2α’Cys336Ser in complex with four inhibitors (4a, 5a, 5b, 10a).
Original languageEnglish
Article number104502
Number of pages12
JournalBioorganic chemistry
Early online date24 Nov 2020
Publication statusPublished - 1 Jan 2021


  • Casein Kinase CK2
  • Protein Kinase PIM1
  • Structural study
  • ATP-Competitive inhibitors

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