Design, synthesis and evaluation of 3-quinoline carboxylic acids as new inhibitors of protein kinase CK2

被引：20

作者：

Syniugin, Anatolii R. ^{[1
]}

Ostrynska, Olga V. ^{[1
]}

Chekanov, Maksym O. ^{[1
]}

Volynets, Galyna P. ^{[1
]}

Starosyla, Sergiy A. ^{[1
]}

Bdzhola, Volodymyr G. ^{[1
]}

Yarmoluk, Sergiy M. ^{[1
]}

机构：

[1] NAS Ukraine, Inst Mol Biol & Genet, Dept Med Chem, 150 Zabolotny Str, UA-03680 Kiev, Ukraine

来源：

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2016年 / 31卷

关键词：

Inhibitor; protein kinase CK2; tetrazolo[1,5-a]quinoline-4-carboxylic acid; 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; REGULATOR; DOCKING;

D O I：

10.1080/14756366.2016.1222584

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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 IC50 in the range from 0.65 to 18.2 mu M were identified. The most active inhibitors were found among tetrazolo-quinoline-4-carboxylic acid and 2-aminoquinoline-3-carboxylic acid derivatives.

引用

页码：160 / 169

页数：10

共 31 条

[1]

[Anonymous], 2005, Patent, Patent No. [W02005/30774 2005

[2]

Al, 200530774]

[3] Unprecedented Selectivity and Structural Determinants of a New Class of Protein Kinase CK2 Inhibitors in Clinical Trials for the Treatment of Cancer [J].

Battistutta, Roberto ;

Cozza, Giorgio ;

Pierre, Fabrice ;

Papinutto, Elena ;

Lolli, Graziano ;

Sarno, Stefania ;

O'Brien, Sean E. ;

Siddiqui-Jain, Adam ;

Haddach, Mustapha ;

Anderes, Kenna ;

Ryckman, David M. ;

Meggio, Flavio ;

Pinna, Lorenzo A. .

BIOCHEMISTRY, 2011, 50 (39) :8478-8488

[4] INHIBITION OF THE FUSION-INDUCING CONFORMATIONAL CHANGE OF INFLUENZA HEMAGGLUTININ BY BENZOQUINONES AND HYDROQUINONES [J].

BODIAN, DL ;

YAMASAKI, RB ;

BUSWELL, RL ;

STEARNS, JF ;

WHITE, JM ;

KUNTZ, ID .

BIOCHEMISTRY, 1993, 32 (12) :2967-2978

[5] Comparative study of several algorithms for flexible ligand docking [J].

Bursulaya, BD ;

Totrov, M ;

Abagyan, R ;

Brooks, CL .

JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN, 2003, 17 (11) :755-763

[6] DOCK 4.0: Search strategies for automated molecular docking of flexible molecule databases [J].

Ewing, TJA ;

Makino, S ;

Skillman, AG ;

Kuntz, ID .

JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN, 2001, 15 (05) :411-428

[7] Subcellular localization of protein kinase CK2 - A key to its function? [J].

Faust, M ;

Montenarh, M .

CELL AND TISSUE RESEARCH, 2000, 301 (03) :329-340

[8] Evaluation of 3-carboxy-4(1H)-quinolones as inhibitors of human protein kinase CK2 [J].

Golub, Andriy G. ;

Yakovenko, Olexander Ya. ;

Bdzhola, Volodymyr G. ;

Sapelkin, Vladislav M. ;

Zien, Piotr ;

Yarmoluk, Sergiy M. .

JOURNAL OF MEDICINAL CHEMISTRY, 2006, 49 (22) :6443-6450

[9] Assay of protein kinases using radiolabeled ATP: a protocol [J].

Hastie, C. James ;

McLauchlan, Hilary J. ;

Cohen, Philip .

NATURE PROTOCOLS, 2006, 1 (02) :968-971

[10] GROMACS 3.0: a package for molecular simulation and trajectory analysis [J].

Lindahl, E ;

Hess, B ;

van der Spoel, D .

JOURNAL OF MOLECULAR MODELING, 2001, 7 (08) :306-317

← 1 2 3 4 →