title: Structure-based design, synthesis, and study of pyrazolo[1,5-a][1,3,5]triazine derivatives as potent inhibitors of protein kinase CK2.
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.
authors.affiliation: Department of Medicinal Chemistry, Polaris Pharmaceuticals Inc., San Diego, CA 92121, USA. zhe.nie@takedasd.com
authors.forename: Zhe
authors.initials: Z
authors.lastname: Nie
authors.forename: Carin
authors.initials: C
authors.lastname: Perretta
authors.forename: Philip
authors.initials: P
authors.lastname: Erickson
authors.forename: Stephen
authors.initials: S
authors.lastname: Margosiak
authors.forename: Robert
authors.initials: R
authors.lastname: Almassy
authors.forename: Jia
authors.initials: J
authors.lastname: Lu
authors.forename: April
authors.initials: A
authors.lastname: Averill
authors.forename: Kraig M
authors.initials: KM
authors.lastname: Yager
authors.forename: Shaosong
authors.initials: S
authors.lastname: Chu
mesh_terms: D001665:Binding Sites; D047390:Casein Kinase II / Q000037:antagonists & inhibitors* / Q000378:metabolism; D045744:Cell Line, Tumor; D018360:Crystallography, X-Ray; D015195:Drug Design; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D047428:Protein Kinase Inhibitors; D047390:Casein Kinase II