Hit generation and exploration:: Imidazo[4,5-b] pyridine derivatives as inhibitors of Aurora kinases

被引：86

作者：

Bavetsias, Vassilios ^{[1
]}

Sun, Chongbo ^{[1
]}

Bouloc, Nathalie ^{[1
]}

Reynisson, Johannes ^{[1
]}

Workman, Paul ^{[1
]}

Linardopoulos, Spiros ^{[1
]}

McDonald, Edward ^{[1
]}

机构：

[1] Inst Canc Res, Canc Res UK Lab, Canc Res UK Ctr Canc Therapeut, Dept Chem, Sutton SM2 5NG, Surrey, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 23期

关键词：

D O I：

10.1016/j.bmcl.2007.09.076

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A hit generation and exploration approach led to the discovery of 31 (2-(4-(6-chloro-2-(4-(dimethylamino) phenyl)-3H-imidazo[4,5-b] pyridin-7-yl) piperazin-1-yl)-N-(thiazol-2-yl) acetamide), a potent, novel inhibitor of Aurora-A, Aurora-B and Aurora-C kinases with IC50 values of 0.042, 0.198 and 0.227 mu M, respectively. Compound 31 inhibits cell proliferation and has good microsomal stability. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：6567 / 6571

页数：5

共 24 条

[21] PHA-680632, a novel aurora kinase inhibitor with potent antitumoral activity [J].

Soncini, Chiara ;

Carpinelli, Patrizia ;

Gianellini, Laura ;

Fancelli, Daniele ;

Vianello, Paola ;

Rusconi, Luisa ;

Storici, Paola ;

Zugnoni, Paola ;

Pesenti, Enrico ;

Croci, Valter ;

Ceruti, Roberta ;

Giorgini, Maria Laura ;

Cappella, Paolo ;

Ballinari, Dario ;

Sola, Francesco ;

Varasi, Mario ;

Bravo, Rodrigo ;

Moll, Juergen .

CLINICAL CANCER RESEARCH, 2006, 12 (13) :4080-4089

[22] High-throughput screening assay for identification of small molecule inhibitors of Aurora2/STK15 kinase [J].

Sun, CB ;

Newbatt, Y ;

Douglas, L ;

Workman, P ;

Aherne, W ;

Linardopoulos, S .

JOURNAL OF BIOMOLECULAR SCREENING, 2004, 9 (05) :391-397

[23]

Tanaka T, 1999, CANCER RES, V59, P2041

[24] A versatile method for the synthesis of benzimidazoles from o-nitroanilines and aldehydes in one step via a reductive cyclization [J].

Yang, DL ;

Fokas, D ;

Li, JZ ;

Yu, LB ;

Baldino, CM .

SYNTHESIS-STUTTGART, 2005, (01) :47-56

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