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生命过程小分子调节剂的研究:Selective Inhibition of Matrix Metalloproteinase Isozymes and in Vivo Protection against ...

  • 关键字: Matrix Metalloproteinase Isozymes 发布者:Dawei Ma, Yongwen Jiang, et. 发布时间:2009-03-03 08:03:50 点击数: 3845次

J. Med. Chem., 2006, 49, 456–458.
Selective Inhibition of Matrix Metalloproteinase Isozymes and in Vivo Protection against Emphysema by Substituted γ-Keto Carboxylic Acids
Dawei Ma, Yongwen Jiang, Fangping Chen, Li-kun Gong, Ke Ding, Yong Xu, Renxiao Wang, Aihua Ge, Jin Ren, Jingya Li, Jia Li, and Qizhuang Ye
State Key Laboratory of Bioorganic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032, China, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China, and Chinese National Center for Drug Screening, Shanghai Institute of Materia Medica, Shanghai Institute for Biological Sciences, Chinese Academy of Sciences, Shanghai 201203, China
 

Abstract. The synthesis and matrix metalloproteinase (MMP) inhibitory activity of a series of γ-keto carboxylic acids are described. Among nine MMP isozymes tested, compound 1j displays selective inhibition of MMP-2, -9, and -12 with IC50 values between 0.20 and 1.51 mM, and in male golden Syrian hamsters, it shows protection against PPE-induced emphysema.