Structure-based design and synthesis of novel macrocyclic pyrazolo[1,5-a][1,3,5]triazine compounds as potent inhibitors of protein kinase CK2 and their anticancer activities
Z. Nie, C. Perretta, P. Ericksin, S. Margosiak, J. Lu, A. Averill, R. Almassy and S. ChuBioorganic & Medicinal Chemistry Letters (2008), Vol. 18 pages 619-623
A series of macrocyclic derivatives has been designed and synthesized based on the X-ray co-crystal structures of pyrazolo[1,5-a] [1,3,5]triazines with corn CK2 (cCK2) protein. Bioassays demonstrated that these macrocyclic pyrazolo[1,5-a][1,3,5]triazine compounds are potent CK2 inihibitors with K9i) around 1.0 nM and strongly inhibit cancer cell growth IC(50) as low as approximately 100 nM.