Structure-based design, synthesis, and study of pyrazolo[1,5-a][1,3,5]triazine derivatives as potent inhibitors of protein kinase CK2.

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Nie Z, Perretta C, Erickson P, Margosiak S, Almassy R, Lu J, Averill A, Yager KM, Chu S

Structure-based design, synthesis, and study of pyrazolo[1,5-a][1,3,5]triazine derivatives as potent inhibitors of protein kinase CK2.

Bioorg Med Chem Lett. 2007 Aug 1;17(15):4191-5. Epub 2007 May 18.

PubMed ID

17540560 [ View in PubMed

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Abstract

The structure-based design, synthesis, and anticancer activity of novel inhibitors of protein kinase CK2 are described. Using pyrazolo[1,5-a][1,3,5]triazine as the core scaffold, a structure-guided series of modifications provided pM inhibitors with microM-level cytotoxic activity in cell-based assays with prostate and colon cancer cell lines.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
2-(4-CHLOROBENZYLAMINO)-4-(PHENYLAMINO)PYRAZOLO[1,5-A][1,3,5]TRIAZINE-8-CARBONITRILE	Casein kinase II subunit alpha	Ki (nM)	5	N/A	N/A	Details
2-(4-ETHYLPIPERAZIN-1-YL)-4-(PHENYLAMINO)PYRAZOLO[1,5-A][1,3,5]TRIAZINE-8-CARBONITRILE	Casein kinase II subunit alpha	Ki (nM)	24	N/A	N/A	Details
2-(CYCLOHEXYLMETHYLAMINO)-4-(PHENYLAMINO)PYRAZOLO[1,5-A][1,3,5]TRIAZINE-8-CARBONITRILE	Casein kinase II subunit alpha	Ki (nM)	8	N/A	N/A	Details
N-(3-(8-CYANO-4-(PHENYLAMINO)PYRAZOLO[1,5-A][1,3,5]TRIAZIN-2-YLAMINO)PHENYL)ACETAMIDE	Casein kinase II subunit alpha	Ki (nM)	0.35	N/A	N/A	Details