Literature DB >> 18793846

Discovery of pyrimidine benzimidazoles as Lck inhibitors: part I.

Guobao Zhang1, Pingda Ren, Nathanael S Gray, Taebo Sim, Yi Liu, Xia Wang, Jianwei Che, Shin-Shay Tian, Mark L Sandberg, Tracy A Spalding, Russell Romeo, Maya Iskandar, Donald Chow, H Martin Seidel, Donald S Karanewsky, Yun He.   

Abstract

A series of 4-amino-6-benzimidazole-pyrimidines was designed to target lymphocyte-specific tyrosine kinase (Lck), a member of the Src kinase family. Highly efficient parallel syntheses were devised to prepare analogues for SAR studies. A number of these 4-amino-6-benzimidazole-pyrimidines exhibited single-digit nanomolar IC(50)s against Lck in biochemical and cellular assays. These 4-amino-6-benzimidazole-pyrimidines represent a new class of tyrosine kinase inhibitors.

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Year:  2008        PMID: 18793846     DOI: 10.1016/j.bmcl.2008.08.104

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


  4 in total

1.  Discovery of Mer specific tyrosine kinase inhibitors for the treatment and prevention of thrombosis.

Authors:  Weihe Zhang; Andrew L McIver; Michael A Stashko; Deborah DeRyckere; Brian R Branchford; Debra Hunter; Dmitri Kireev; Michael J Miley; Jacqueline Norris-Drouin; Wendy M Stewart; Minjung Lee; Susan Sather; Yingqiu Zhou; Jorge A Di Paola; Mischa Machius; William P Janzen; H Shelton Earp; Douglas K Graham; Stephen V Frye; Xiaodong Wang
Journal:  J Med Chem       Date:  2013-11-20       Impact factor: 7.446

2.  Ethyl 1-tert-butyl-2-(4-hydr-oxy-3-methoxy-phen-yl)-1H-benzimidazole-5-carboxyl-ate.

Authors:  Natarajan Arumugam; Aisyah Saad Abdul Rahim; Hasnah Osman; Mohd Mustaqim Rosli; Hoong-Kun Fun
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-04-10

3.  Pseudo-cyclization through intramolecular hydrogen bond enables discovery of pyridine substituted pyrimidines as new Mer kinase inhibitors.

Authors:  Weihe Zhang; Dehui Zhang; Michael A Stashko; Deborah DeRyckere; Debra Hunter; Dmitri Kireev; Michael J Miley; Christopher Cummings; Minjung Lee; Jacqueline Norris-Drouin; Wendy M Stewart; Susan Sather; Yingqiu Zhou; Gregory Kirkpatrick; Mischa Machius; William P Janzen; H Shelton Earp; Douglas K Graham; Stephen V Frye; Xiaodong Wang
Journal:  J Med Chem       Date:  2013-11-20       Impact factor: 7.446

4.  Ethyl 1-phenyl-2-[4-(trifluoro-meth-oxy)phen-yl]-1H-benzimidazole-5-carboxyl-ate.

Authors:  Yeong Keng Yoon; Mohamed Ashraf Ali; Tan Soo Choon; Suhana Arshad; Ibrahim Abdul Razak
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-08-15
  4 in total

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