Literature DB >> 16997556

The development of 2-benzimidazole substituted pyrimidine based inhibitors of lymphocyte specific kinase (Lck).

Mark Sabat1, John C VanRens, Matthew J Laufersweiler, Todd A Brugel, Jennifer Maier, Adam Golebiowski, Biswanath De, Vijayasurian Easwaran, Lily C Hsieh, Richard L Walter, Marlene J Mekel, Artem Evdokimov, Michael J Janusz.   

Abstract

This communication details the synthesis, biological activity, and binding mode of a novel class of 2-benzimidazole substituted pyrimidines. The most potent analogs disclosed showed low nanomolar activity for the inhibition of Lck kinase and a representative analog was co-crystallized with Hck (a structurally related member of the Src family kinases).

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Year:  2006        PMID: 16997556     DOI: 10.1016/j.bmcl.2006.08.132

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


  4 in total

1.  Flexibility and charge asymmetry in the activation loop of Src tyrosine kinases.

Authors:  Nilesh K Banavali; Benoît Roux
Journal:  Proteins       Date:  2009-02-01

2.  Involvement of conformational isomerism in the complexity of the crystal network of 1-(4-nitrophenyl)-1H-1,3-benzimidazole derivatives driven by C-H...A (A = NO2, Npy and π) and orthogonal Npy...NO2 and ONO...Csp2 interactions.

Authors:  Mónica I García-Aranda; Carlos Z Gómez-Castro; Efrén V García-Báez; Yolanda Gómez Y Gómez; José L Castrejón-Flores; Itzia I Padilla-Martínez
Journal:  Acta Crystallogr C Struct Chem       Date:  2018-03-07       Impact factor: 1.172

3.  Kinase inhibitors for the treatment of inflammatory and autoimmune disorders.

Authors:  Shripad S Bhagwat
Journal:  Purinergic Signal       Date:  2008-06-21       Impact factor: 3.765

4.  Src-family kinases negatively regulate NFAT signaling in resting human T cells.

Authors:  Alan Baer; Winston Colon-Moran; Jinhua Xiang; Jack T Stapleton; Nirjal Bhattarai
Journal:  PLoS One       Date:  2017-10-26       Impact factor: 3.240

  4 in total

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