Chojnacki, K.; Lindenblatt, D.; Winska, P.; Wielechowska, M.; Toelzer, C.; Niefind, K.; Bretner, M. published the artcile< Synthesis, biological properties and structural study of new halogenated azolo[4,5-b]pyridines as inhibitors of CK2 kinase>, SDS of cas: 92276-38-5, the main research area is halogenated azolopyridine synthesis anticancer CK2 kinase inhibition; ATP-Competitive inhibitors; Casein Kinase CK2; Protein Kinase PIM1; Structural study.
The new halogenated 1H-triazolo[4,5-b]pyridines and 1H-imidazo[4,5-b]pyridines were synthesized as analogs 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 I-III with IC50 values 2.56, 3.82 and 3.26μM resp. 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 I-III were obtained. In addition, new protocol was used to obtain high-resolution crystal structures of CK2α’Cys336Ser in complex with four inhibitors I-IV.
Bioorganic Chemistry published new progress about Crystal structure. 92276-38-5 belongs to class triazoles, and the molecular formula is C5H3BrN4, SDS of cas: 92276-38-5.
Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics