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

Bioorganic Chemistry(2018)

引用 19|浏览19
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摘要
•A new alkylamino-TBBi and TBBt derivatives were synthesized.•The TBBi derivatives 8b-c inhibit the activity of protein kinases: CK2 holoenzyme and the PIM1 as effectively as TBBi, while the derivatives of 2MeTBBi, compounds 14a-b exerted superior inhibition of PIM1 kinase.•They reduce the viability of cancer cells.•Derivatives of 2MeTBBi, 14a-b, inhibit the viability of tumour cells even more effectively than the approved for clinical trials CK2 inhibitor CX-4945.•The 3D-structures of the CK2α1-335/8b complex were obtained.
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关键词
Casein kinase 2 CK2,Protein kinase PIM1,ATP-competitive inhibitors,Antiproliferative activity,Structural study
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