Literature DB >> 14592495

Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56(Lck).

John Wityak1, Jagabandhu Das, Robert V Moquin, Zhongqi Shen, James Lin, Ping Chen, Arthur M Doweyko, Sidney Pitt, Suhong Pang, Ding Ren Shen, Qiong Fang, Henry F de Fex, Gary L Schieven, Steven B Kanner, Joel C Barrish.   

Abstract

A novel series of 2-amino-5-carboxamidothiazoles were identified as inhibitors of Lck. Structure-activity studies demonstrate the structural requirements for potent Lck activity. Cyclopropylamide 11d is a potent Lck inhibitor having sub-micromolar activity in a PBL proliferation assay.

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Year:  2003        PMID: 14592495     DOI: 10.1016/j.bmcl.2003.08.054

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


  2 in total

1.  A type-II kinase inhibitor capable of inhibiting the T315I "gatekeeper" mutant of Bcr-Abl.

Authors:  Hwan Geun Choi; Pingda Ren; Francisco Adrian; Fangxian Sun; Hyun Soo Lee; Xia Wang; Qiang Ding; Guobao Zhang; Yongping Xie; Jianming Zhang; Yi Liu; Tove Tuntland; Markus Warmuth; Paul W Manley; Jürgen Mestan; Nathanael S Gray; Taebo Sim
Journal:  J Med Chem       Date:  2010-08-12       Impact factor: 7.446

2.  Synthesis and biological activity of 3-[phenyl(1,3-thiazol-2-yl)-amino]propanoic acids and their derivatives.

Authors:  Vytautas Mickevičius; Aušra Voskienė; Ilona Jonuškienė; Ramūnė Kolosej; Jūratė Šiugždaitė; Petras Rimantas Venskutonis; Rita Kazernavičiūtė; Zita Brazienė; Elena Jakienė
Journal:  Molecules       Date:  2013-12-05       Impact factor: 4.411

  2 in total

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