title: Design, synthesis and evaluation of 3-quinoline carboxylic acids as new inhibitors of protein kinase CK2.
abstract: In this article, the derivatives of 3-quinoline carboxylic acid were studied as inhibitors of protein kinase CK2. Forty-three new compounds were synthesized. Among them 22 compounds inhibiting CK2 with IC50in the range from 0.65 to 18.2 μM were identified. The most active inhibitors were found among tetrazolo-quinoline-4-carboxylic acid and 2-aminoquinoline-3-carboxylic acid derivatives.
authors: a Department of Medicinal Chemistry , Institute of Molecular Biology and Genetics, NAS of Ukraine , Kyiv , Ukraine.
authors: Anatolii R
authors: AR
authors: Syniugin
authors: a Department of Medicinal Chemistry , Institute of Molecular Biology and Genetics, NAS of Ukraine , Kyiv , Ukraine.
authors: Olga V
authors: OV
authors: Ostrynska
authors: a Department of Medicinal Chemistry , Institute of Molecular Biology and Genetics, NAS of Ukraine , Kyiv , Ukraine.
authors: Maksym O
authors: MO
authors: Chekanov
authors: a Department of Medicinal Chemistry , Institute of Molecular Biology and Genetics, NAS of Ukraine , Kyiv , Ukraine.
authors: Galyna P
authors: GP
authors: Volynets
authors: a Department of Medicinal Chemistry , Institute of Molecular Biology and Genetics, NAS of Ukraine , Kyiv , Ukraine.
authors: Sergiy A
authors: SA
authors: Starosyla
authors: a Department of Medicinal Chemistry , Institute of Molecular Biology and Genetics, NAS of Ukraine , Kyiv , Ukraine.
authors: Volodymyr G
authors: VG
authors: Bdzhola
authors: a Department of Medicinal Chemistry , Institute of Molecular Biology and Genetics, NAS of Ukraine , Kyiv , Ukraine.
authors: Sergiy M
authors: SM
authors: Yarmoluk
mesh_terms: D002264:Carboxylic Acids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D047390:Casein Kinase II / Q000037:antagonists & inhibitors* / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D006801:Humans; D062105:Molecular Docking Simulation; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D002264:Carboxylic Acids; D047428:Protein Kinase Inhibitors; D011804:Quinolines; D047390:Casein Kinase II
keywords: 2-aminoquinoline-3-carboxylic acid; 2-chloroquinoline-3-carboxylic acid; 2-oxo-1,2-dihydroquinoline-3-carboxylic acid; 5-oxo-2,3-dihydro-1H,5H-pyrido[3,2,1-ij]quinoline-6-carboxylic acid; Inhibitor; protein kinase CK2; tetrazolo[1,5-a]quinoline-4-carboxylic acid