Literature DB >> 17937984

2-Aryl benzimidazoles featuring alkyl-linked pendant alcohols and amines as inhibitors of checkpoint kinase Chk2.

Danielle K Neff1, Alice Lee-Dutra, Jonathan M Blevitt, Frank U Axe, Michael D Hack, Johnathan C Buma, Raymond Rynberg, Anders Brunmark, Lars Karlsson, J Guy Breitenbucher.   

Abstract

A series of benzimidazole compounds containing pendant alcohol and amine moieties was found to be active against checkpoint kinase Chk2. These compounds were prepared to examine a potential hydrogen bond interaction with an active site residue and to investigate replacement of a biaryl linker with an aliphatic system in an effort to improve solubility.

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Year:  2007        PMID： 17937984     DOI： 10.1016/j.bmcl.2007.09.098

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


  7 in total

1.  Crystal structure of checkpoint kinase 2 in complex with NSC 109555, a potent and selective inhibitor.

Authors:  George T Lountos; Joseph E Tropea; Di Zhang; Andrew G Jobson; Yves Pommier; Robert H Shoemaker; David S Waugh
Journal:  Protein Sci       Date:  2009-01       Impact factor: 6.725

Review 2.  Structure-based design, discovery and development of checkpoint kinase inhibitors as potential anticancer therapies.

Authors:  Thomas P Matthews; Alan M Jones; Ian Collins
Journal:  Expert Opin Drug Discov       Date:  2013-04-18       Impact factor: 6.098

Review 3.  Imidazoles as potential anticancer agents.

Authors:  Imran Ali; Mohammad Nadeem Lone; Haasan Y Aboul-Enein
Journal:  Medchemcomm       Date:  2017-04-13       Impact factor: 3.597

4.  Benzimidazole inhibitors of the protein kinase CHK2: clarification of the binding mode by flexible side chain docking and protein-ligand crystallography.

Authors:  Cornelis Matijssen; M Cris Silva-Santisteban; Isaac M Westwood; Samerene Siddique; Vanessa Choi; Peter Sheldrake; Rob L M van Montfort; Julian Blagg
Journal:  Bioorg Med Chem       Date:  2012-09-21       Impact factor: 3.641

5.  Fragment-based screening maps inhibitor interactions in the ATP-binding site of checkpoint kinase 2.

Authors:  M Cris Silva-Santisteban; Isaac M Westwood; Kathy Boxall; Nathan Brown; Sam Peacock; Craig McAndrew; Elaine Barrie; Meirion Richards; Amin Mirza; Antony W Oliver; Rosemary Burke; Swen Hoelder; Keith Jones; G Wynne Aherne; Julian Blagg; Ian Collins; Michelle D Garrett; Rob L M van Montfort
Journal:  PLoS One       Date:  2013-06-12       Impact factor: 3.240

6.  A benzimidazole derivative exhibiting antitumor activity blocks EGFR and HER2 activity and upregulates DR5 in breast cancer cells.

Authors:  B Chu; F Liu; L Li; C Ding; K Chen; Q Sun; Z Shen; Y Tan; C Tan; Y Jiang
Journal:  Cell Death Dis       Date:  2015-03-12       Impact factor: 8.469

7.  Molecular docking studies of benzimidazopyrimidine and coumarin substituted benzimidazopyrimidine derivatives: As potential human Aurora A kinase inhibitors.

Authors:  Kallimeledoddi B Puttaraju; Sankanahally Srinivasshetty Mahesh; Kalegowda Shivashankar; Neratur Krishnappagowda Lokanath; Mahendra Madegowda
Journal:  Bioinformation       Date:  2014-05-20
  7 in total

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