Das Jagabandhu, Moquin Robert V, Lin James, Liu Chunjian, Doweyko Arthur M, DeFex Henry F, Fang Qiong, Pang Suhong, Pitt Sidney, Shen Ding Ren, Schieven Gary L, Barrish Joel C, Wityak John
Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA.
Bioorg Med Chem Lett. 2003 Aug 4;13(15):2587-90. doi: 10.1016/s0960-894x(03)00511-0.
A series of structurally novel benzothiazole based small molecule inhibitors of p56(lck) was prepared to elucidate their structure-activity relationships (SAR), selectivity and cell activity in the T-cell proliferation assay. BMS-350751 (2) and BMS-358233 (3) are identified as potent Lck inhibitors with excellent cellular activities against T-cell proliferation.
制备了一系列基于苯并噻唑结构的新型p56(lck)小分子抑制剂，以阐明其构效关系（SAR）、选择性以及在T细胞增殖试验中的细胞活性。BMS-350751（2）和BMS-358233（3）被鉴定为有效的Lck抑制剂，对T细胞增殖具有优异的细胞活性。
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