title: Design and synthesis of CK2 inhibitors.
abstract: A series of new polybrominated benzimidazoles and benzotriazoles has been synthesized and their influence on the activity of protein kinase CK2 was evaluated. It was revealed that the most active inhibitors are those with methyl or ethyl substituent at benzene ring, namely 5,6,7-tribromo-4-methyl-1H-benzotriazole (38, IC(50) 0.51 μM) and 5,6,7-tribromo-4-ethyl-1H-benzotriazole (40, IC(50) 0.16 μM). The derivatives with large aromatic or heterocyclic substituents connected to benzimidazole or benzotriazole scaffold appeared to be less potent inhibitors.
authors.affiliation: Institute of Biochemistry and Biophysics, PAS, Pawińskiego 5A, 02-106 Warszawa, Poland.
authors.forename: Małgorzata
authors.initials: M
authors.lastname: Makowska
authors.forename: Edyta
authors.initials: E
authors.lastname: Łukowska-Chojnacka
authors.forename: Patrycja
authors.initials: P
authors.lastname: Wińska
authors.forename: Agnieszka
authors.initials: A
authors.lastname: Kuś
authors.forename: Aleksandra
authors.initials: A
authors.lastname: Bilińska-Chomik
authors.forename: Maria
authors.initials: M
authors.lastname: Bretner
mesh_terms: D001562:Benzimidazoles / Q000737:chemistry / Q000494:pharmacology; D047390:Casein Kinase II / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015195:Drug Design; D006801:Humans; D020128:Inhibitory Concentration 50; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D014230:Triazoles / Q000737:chemistry / Q000494:pharmacology
chemical_list: C475924:4,5,6,7-tetrabromobenzimidazole; C405354:4,5,6,7-tetrabromobenzotriazole; D001562:Benzimidazoles; D047428:Protein Kinase Inhibitors; D014230:Triazoles; D047390:Casein Kinase II