吡咯衍生物作为淋巴细胞特异性激酶的有效抑制剂：结构、合成和 SAR。
Pyrrole derivatives as potent inhibitors of lymphocyte-specific kinase: 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):108-11. doi: 10.1016/j.bmcl.2009.11.014. Epub 2009 Nov 12.
PMID:19945869
Abstract
We have described the synthesis, enzyme inhibitory activity, structure-activity relationships, and proposed binding mode of a novel series of pyrrole derivatives as lymphocyte-specific kinase (Lck) inhibitors. The most potent analogs exhibited good enzyme inhibitory activity (IC(50)s <10nM) for Lck kinase inhibition.
摘要
我们描述了一系列新型吡咯衍生物作为淋巴细胞特异性激酶（Lck）抑制剂的合成、酶抑制活性、构效关系和建议的结合模式。最有效的类似物对 Lck 激酶抑制表现出良好的酶抑制活性（IC50<10nM）。
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