稠合吡唑衍生物作为淋巴细胞特异性激酶（Lck）的有效抑制剂：结构、合成和 SAR。
Ring-fused pyrazole derivatives as potent inhibitors of lymphocyte-specific kinase (Lck): Structure, synthesis, and SAR.
机构信息
Medicinal Research Laboratories, Taisho Pharmaceutical Co., Ltd, 403, Yoshino-Cho 1-Chome, Kita-Ku, Saitama-Shi, Saitama 331-9530, Japan.
出版信息
Bioorg Med Chem Lett. 2010 Jan 1;20(1):112-6. doi: 10.1016/j.bmcl.2009.11.013. Epub 2009 Nov 12.
PMID:19945867
Abstract
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 (IC(50)s <1nM) as well as excellent cellular activity against mixed lymphocyte reaction (MLR) (IC(50)s <1nM).
摘要
我们已经鉴定了一系列新型的稠合吡唑衍生物作为淋巴细胞特异性激酶（Lck）抑制剂。最有效的类似物具有良好的酶抑制活性（IC50<1nM）以及针对混合淋巴细胞反应（MLR）的优异细胞活性（IC50<1nM）。
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