Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1365379 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
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 inhibitors with Ki around 1.0 nM and strongly inhibit cancer cell growth with IC50 as low as ∼100 nM.
Graphical abstractA 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 inhibitors with Ki around 1.0 nM and they strongly inhibit cancer cell growth with IC50 as low as ∼100 nM.Figure optionsDownload full-size imageDownload as PowerPoint slide