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Ring-fused pyrazole derivatives as potent inhibitors of lymphocyte-specific kinase (Lck): Structure, synthesis, and SAR

cappuccinolin1 添加于 2011-8-15 16:49 | 1724 次阅读 | 0 个评论

作者
Takayama T, Umemiya H, Amada H, Yabuuchi T, Koami T, Shiozawa F, Oka Y, Takaoka A, Yamaguchi A, Endo M, Sato M
摘要
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).
详细资料
- 文献种类:期刊
- 期刊名称: Bioorganic & Medicinal Chemistry Letters
- 期刊缩写: Bioorg Med Chem Lett
- 期卷页: 2010年第20卷第1期 112-116页
- 地址: Medicinal Research Laboratories, Taisho Pharmaceutical Co., Ltd, 403, Yoshino-Cho 1-Chome, Kita-Ku, Saitama-Shi, Saitama 331-9530, Japan. tetsuo.takayama@po.rd.taisho.co.jp
- ISBN: 0960-894X
- 备注:PMID:19945867
标签

Ring-fused pyrazole
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Ring-fused pyrazole