Literature DB >> 20674350

Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.

David B Belanger1, Patrick J Curran, Alan Hruza, Johannes Voigt, Zhaoyang Meng, Amit K Mandal, M Arshad Siddiqui, Andrea D Basso, Kimberly Gray.   

Abstract

The synthesis and structure-activity relationships (SAR) of novel, potent imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors are described. The X-ray crystal structure of imidazo[1,2-a]pyrazine Aurora inhibitor 1j is disclosed. Compound 10i was identified as lead compound with a promising overall profile. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20674350     DOI： 10.1016/j.bmcl.2010.07.008

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


  4 in total

1.  Development of o-chlorophenyl substituted pyrimidines as exceptionally potent aurora kinase inhibitors.

Authors:  Matthew P Martin; Yunting Luo; Roberta Pireddu; Hua Yang; Harsukh Gevariya; Harshani R Lawrence; Sevil Ozcan; Jin-Yi Zhu; Robert Kendig; Mercedes Rodriguez; Roy Elias; Jin Q Cheng; Saïd M Sebti; Ernst Schonbrunn; Nicholas J Lawrence
Journal:  J Med Chem       Date:  2012-08-30       Impact factor: 7.446

2.  A bulky biaryl phosphine ligand allows for palladium-catalyzed amidation of five-membered heterocycles as electrophiles.

Authors:  Mingjuan Su; Stephen L Buchwald
Journal:  Angew Chem Int Ed Engl       Date:  2012-03-30       Impact factor: 15.336

3.  Discovery of Imidazo[1,2-a]pyrazines and Pyrazolo[1,5-c]pyrimidines as TARP γ-8 Selective AMPAR Negative Modulators.

Authors:  Brad M Savall; Dongpei Wu; Devin M Swanson; Mark Seierstad; Nyantsz Wu; Jorge Vives Martinez; Beatriz García Olmos; Brian Lord; Kevin Coe; Tatiana Koudriakova; Timothy W Lovenberg; Nicholas I Carruthers; Michael P Maher; Michael K Ameriks
Journal:  ACS Med Chem Lett       Date:  2018-12-26       Impact factor: 4.345

4.  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
  4 in total

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