Das Jagabandhu, Lin James, Moquin Robert V, Shen Zhongqi, Spergel Steven H, Wityak John, Doweyko Arthur M, DeFex Henry F, Fang Qiong, Pang Suhong, Pitt Sidney, Shen Ding Ren, Schieven Gary L, Barrish Joel C
Bristol-Myers Squibb Pharmaceutical Research Institute, 08543-4000, Princeton, NJ, USA.
Bioorg Med Chem Lett. 2003 Jul 7;13(13):2145-9. doi: 10.1016/s0960-894x(03)00380-9.
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.
制备了一系列基于苯并噻唑的结构新颖的p56(lck)小分子抑制剂，以阐明它们在T细胞增殖试验中的构效关系（SARs）、选择性和细胞活性。BMS-243117（化合物2）被鉴定为一种强效且选择性的Lck抑制剂，对T细胞增殖具有良好的细胞活性（IC(50)=1.1 microM）。
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