Literature DB >> 20833547

Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells.

Nathalie Bouloc1, Jonathan M Large, Magda Kosmopoulou, Chongbo Sun, Amir Faisal, Mizio Matteucci, Jóhannes Reynisson, Nathan Brown, Butrus Atrash, Julian Blagg, Edward McDonald, Spiros Linardopoulos, Richard Bayliss, Vassilios Bavetsias.   

Abstract

Co-crystallisation of the imidazo[1,2-a]pyrazine derivative 15 (3-chloro-N-(4-morpholinophenyl)-6-(pyridin-3-yl)imidazo[1,2-a]pyrazin-8-amine) with Aurora-A provided an insight into the interactions of this class of compound with Aurora kinases. This led to the design and synthesis of potent Aurora-A inhibitors demonstrating up to 70-fold selectivity in cell-based Aurora kinase pharmacodynamic biomarker assays.
Copyright © 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20833547     DOI： 10.1016/j.bmcl.2010.08.091

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


  10 in total

1.  Combined 3D-QSAR modeling and molecular docking studies on pyrrole-indolin-2-ones as Aurora A kinase inhibitors.

Authors:  Yong Ai; Shao-Teng Wang; Ping-Hua Sun; Fa-Jun Song
Journal:  Int J Mol Sci       Date:  2011-03-01       Impact factor: 5.923

2.  2- and 3-substituted imidazo[1,2-a]pyrazines as inhibitors of bacterial type IV secretion.

Authors:  James R Sayer; Karin Walldén; Thomas Pesnot; Frederick Campbell; Paul J Gane; Michela Simone; Hans Koss; Floris Buelens; Timothy P Boyle; David L Selwood; Gabriel Waksman; Alethea B Tabor
Journal:  Bioorg Med Chem       Date:  2014-09-28       Impact factor: 3.641

3.  Detection of Ligand-induced Conformational Changes in the Activation Loop of Aurora-A Kinase by PELDOR Spectroscopy.

Authors:  Selena G Burgess; Maria Grazia Concilio; Richard Bayliss; Alistair J Fielding
Journal:  ChemistryOpen       Date:  2016-11-11       Impact factor: 2.911

Review 4.  The azaindole framework in the design of kinase inhibitors.

Authors:  Jean-Yves Mérour; Frédéric Buron; Karen Plé; Pascal Bonnet; Sylvain Routier
Journal:  Molecules       Date:  2014-11-28       Impact factor: 4.411

Review 5.  Synthetic approaches and pharmaceutical applications of chloro-containing molecules for drug discovery: A critical review.

Authors:  Wan-Yin Fang; L Ravindar; K P Rakesh; H M Manukumar; C S Shantharam; Njud S Alharbi; Hua-Li Qin
Journal:  Eur J Med Chem       Date:  2019-04-10       Impact factor: 6.514

6.  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

Review 7.  On the molecular mechanisms of mitotic kinase activation.

Authors:  Richard Bayliss; Andrew Fry; Tamanna Haq; Sharon Yeoh
Journal:  Open Biol       Date:  2012-11       Impact factor: 6.411

8.  7-(Pyrazol-4-yl)-3H-imidazo[4,5-b]pyridine-based derivatives for kinase inhibition: Co-crystallisation studies with Aurora-A reveal distinct differences in the orientation of the pyrazole N1-substituent.

Authors:  Vassilios Bavetsias; Yolanda Pérez-Fuertes; Patrick J McIntyre; Butrus Atrash; Magda Kosmopoulou; Lisa O'Fee; Rosemary Burke; Chongbo Sun; Amir Faisal; Katherine Bush; Sian Avery; Alan Henley; Florence I Raynaud; Spiros Linardopoulos; Richard Bayliss; Julian Blagg
Journal:  Bioorg Med Chem Lett       Date:  2015-08-06       Impact factor: 2.823

9.  A Cell Biologist's Field Guide to Aurora Kinase Inhibitors.

Authors:  Christian O de Groot; Judy E Hsia; John V Anzola; Amir Motamedi; Michelle Yoon; Yao Liang Wong; David Jenkins; Hyun J Lee; Mallory B Martinez; Robert L Davis; Timothy C Gahman; Arshad Desai; Andrew K Shiau
Journal:  Front Oncol       Date:  2015-12-21       Impact factor: 6.244

10.  Aurora isoform selectivity: design and synthesis of imidazo[4,5-b]pyridine derivatives as highly selective inhibitors of Aurora-A kinase in cells.

Authors:  Vassilios Bavetsias; Amir Faisal; Simon Crumpler; Nathan Brown; Magda Kosmopoulou; Amar Joshi; Butrus Atrash; Yolanda Pérez-Fuertes; Jessica A Schmitt; Katherine J Boxall; Rosemary Burke; Chongbo Sun; Sian Avery; Katherine Bush; Alan Henley; Florence I Raynaud; Paul Workman; Richard Bayliss; Spiros Linardopoulos; Julian Blagg
Journal:  J Med Chem       Date:  2013-11-06       Impact factor: 7.446
  10 in total

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