Molecular design, synthesis, and structure–Activity relationships leading to the potent and selective p56lck inhibitor BMS-243117
2003; Elsevier BV; Volume: 13; Issue: 13 Linguagem: Inglês
10.1016/s0960-894x(03)00380-9
ISSN1464-3405
AutoresJagabandhu Das, James C. 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,
Tópico(s)NF-κB Signaling Pathways
ResumoA 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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