Literature DB >> 17933533

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

Vassilios Bavetsias1, Chongbo Sun, Nathalie Bouloc, Jóhannes Reynisson, Paul Workman, Spiros Linardopoulos, Edward McDonald.   

Abstract

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 IC(50) values of 0.042, 0.198 and 0.227microM, respectively. Compound 31 inhibits cell proliferation and has good microsomal stability.

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Year:  2007        PMID： 17933533     DOI： 10.1016/j.bmcl.2007.09.076

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  14 in total

1.  3D-QSAR and molecular docking studies of azaindole derivatives as Aurora B kinase inhibitors.

Authors:  Ping Lan; Wan-Na Chen; Ping-Hua Sun; Wei-Min Chen
Journal:  J Mol Model       Date:  2010-08-11       Impact factor: 1.810

2.  Synthesis of N-Substituted 3-Amino-4-halopyridines: A Sequential Boc-Removal/Reductive Amination Mediated by Brønsted and Lewis Acids.

Authors:  Christopher A Wilhelmsen; Alexandre D C Dixon; John D Chisholm; Daniel A Clark
Journal:  J Org Chem       Date:  2018-01-19       Impact factor: 4.354

3.  3-Benzyl-6-bromo-1H-imidazo[4,5-b]pyridin-2(3H)-one.

Authors:  Youssef Kandri Rodi; Amal Haoudi; Frédéric Capet; Ahmed Mazzah; El Mokhtar Essassi; Lahcen El Ammari
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-05-25

4.  Selective FLT3 inhibition of FLT3-ITD+ acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patterns.

Authors:  A S Moore; A Faisal; D Gonzalez de Castro; V Bavetsias; C Sun; B Atrash; M Valenti; A de Haven Brandon; S Avery; D Mair; F Mirabella; J Swansbury; A D J Pearson; P Workman; J Blagg; F I Raynaud; S A Eccles; S Linardopoulos
Journal:  Leukemia       Date:  2012-02-22       Impact factor: 11.528

5.  6-Bromo-3-methyl-2-phenyl-3H-imidazo[4,5-b]pyridine.

Authors:  Younes Ouzidan; El Mokhtar Essassi; Santiago V Luis; Michael Bolte; Lahcen El Ammari
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-06-18

6.  3-[(1-Benzyl-1H-1,2,3-triazol-5-yl)meth-yl]-6-bromo-2-phenyl-3H-imidazo[4,5-b]pyridine.

Authors:  Younes Ouzidan; Youssef Kandri Rodi; Frank R Fronczek; Ramaiyer Venkatraman; El Mokhtar Essassi; Lahcen El Ammari
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-03-15

7.  1-Acetyl-6-bromo-1H-imidazo[4,5-b]pyridin-2(3H)-one.

Authors:  Siham Dahmani; Youssef Kandri Rodi; Santiago V Luis; El Mokhtar Essassi; Lahcen El Ammari
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-05-11

8.  3-Allyl-6-bromo-1H-imidazo[4,5-b]pyridin-2(3H)-one.

Authors:  Siham Dahmani; Youssef Kandri Rodi; Santiago V Luis; Michael Bolte; Lahcen El Ammari
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-07-09

9.  1,3-Diallyl-6-bromo-1H-imidazo[4,5-b]pyridin-2(3H)-one.

Authors:  Siham Dahmani; Youssef Kandri Rodi; Santiago V Luis; Michael Bolte; Lahcen El Ammari
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-07-09

10.  Optimization of imidazo[4,5-b]pyridine-based kinase inhibitors: identification of a dual FLT3/Aurora kinase inhibitor as an orally bioavailable preclinical development candidate for the treatment of acute myeloid leukemia.

Authors:  Vassilios Bavetsias; Simon Crumpler; Chongbo Sun; Sian Avery; Butrus Atrash; Amir Faisal; Andrew S Moore; Magda Kosmopoulou; Nathan Brown; Peter W Sheldrake; Katherine Bush; Alan Henley; Gary Box; Melanie Valenti; Alexis de Haven Brandon; Florence I Raynaud; Paul Workman; Suzanne A Eccles; Richard Bayliss; Spiros Linardopoulos; Julian Blagg
Journal:  J Med Chem       Date:  2012-10-08       Impact factor: 7.446
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