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 |
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Authors: | Nie Zhe Perretta Carin Erickson Philip Margosiak Stephen Lu Jia Averill April Almassy Robert Chu Shaosong |
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Institution: | Department of Medicinal Chemistry, Polaris Pharmaceuticals Inc., San Diego, CA 92121, USA. zhe.nie@takedasd.com |
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Abstract: | A series of macrocyclic derivatives has been designed and synthesized based on the X-ray co-crystal structures of pyrazolo1,5-a] 1,3,5]triazines with corn CK2 (cCK2) protein. Bioassays demonstrated that these macrocyclic pyrazolo1,5-a] 1,3,5]triazine compounds are potent CK2 inhibitors with K(i) around 1.0 nM and strongly inhibit cancer cell growth with IC(50) as low as approximately 100 nM. |
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