Ring-fused pyrazole derivatives as potent inhibitors of lymphocyte-specific kinase (Lck): Structure, synthesis, and SAR.
Ring-fused pyrazole derivatives as potent inhibitors of lymphocyte-specific kinase (Lck): Structure, synthesis, and SAR.
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DOI：
10.1016/j.bmcl.2009.11.013
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发表时间：
2010
影响因子：
2.7
通讯作者：
Tetsuo Takayama;H. Umemiya;Hideaki Amada;Tetsuya Yabuuchi;T. Koami;Fumiyasu Shiozawa;Yusuke Oka;A. Takaoka;Akie Yamaguchi;Mayumi Endo;Masakazu Sato
中科院分区：
文献类型：
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作者：
Tetsuo Takayama;H. Umemiya;Hideaki Amada;Tetsuya Yabuuchi;T. Koami;Fumiyasu Shiozawa;Yusuke Oka;A. Takaoka;Akie Yamaguchi;Mayumi Endo;Masakazu Sato
我们已经确定了一个新的系列环稠合吡唑衍生物作为淋巴细胞特异性激酶（LCK）抑制剂。最有效的类似物表现出良好的酶抑制活性（IC 50 <1nM）以及对混合淋巴细胞反应（MLR）的优异细胞活性（IC 50 <1nM）。
We have identified a novel series of ring-fused pyrazole derivatives as lymphocyte-specific kinase (Lck) inhibitors. The most potent analogs exhibited good enzyme inhibitory activity (IC50s <1nM) as well as excellent cellular activity against mixed lymphocyte reaction (MLR) (IC50s <1nM).