Molecular design, synthesis, and structure-Activity relationships leading to the potent and selective p56(lck) inhibitor BMS-243117

  • Bioorg Med Chem Lett. 2003 Jul 7;13(13):2145-9. doi: 10.1016/s0960-894x(03)00380-9.
Jagabandhu Das  1 ,  James Lin ,  Robert V Moquin ,  Zhongqi Shen ,  Steven H Spergel ,  John Wityak ,  Arthur M Doweyko ,  Henry F DeFex ,  Qiong Fang ,  Suhong Pang ,  Sidney Pitt ,  Ding Ren Shen ,  Gary L Schieven ,  Joel C Barrish
Affiliations
  • 1. Bristol-Myers Squibb Pharmaceutical Research Institute, 08543-4000, Princeton, NJ, USA. [email protected]
PMID: 12798323 DOI: 10.1016/s0960-894x(03)00380-9
Abstract

A series of structurally novel benzothiazole based small molecule inhibitors of p56(Lck) were prepared to elucidate their structure-activity relationships (SARs), selectivity and cell activity in the T-cell proliferation assay. BMS-243117 (compound 2) is identified as a potent, and selective Lck Inhibitor with good cellular activity (IC(50)=1.1 microM) against T-cell proliferation.

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