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

Autor:	Robert Almassy, Stephen Margosiak, Kraig M. Yager, Shaosong Chu, Carin L. Perretta, April Averill, Erickson Philip Eugene, Zhe Nie, Jia Lu
Rok vydání:	2007
Předmět:	Models Molecular Stereochemistry Clinical Biochemistry Pharmaceutical Science Crystallography X-Ray Biochemistry Chemical synthesis chemistry.chemical_compound 1 3 5-Triazine Cell Line Tumor Drug Discovery Transferase Humans Cytotoxicity Casein Kinase II Molecular Biology Protein Kinase Inhibitors Triazine chemistry.chemical_classification Binding Sites biology Molecular Structure Organic Chemistry Enzyme chemistry Enzyme inhibitor Drug Design biology.protein Molecular Medicine Signal transduction
Zdroj:	Bioorganicmedicinal chemistry letters. 17(15)
ISSN:	0960-894X
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::21f2d545a2888fd96bc3548574040451 https://pubmed.ncbi.nlm.nih.gov/17540560 Zobrazit plný text záznamu Full Text from ScienceDirect