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

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

Affiliation

  • 1 Bristol-Myers Squibb Pharmaceutical Research Institute, 08543-4000, Princeton, NJ, USA. jagabandhu.das@bms.com
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.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-120622
    Lck Inhibitor
    Src