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[Design, synthesis and activity evaluation of novel matrix metalloproteinases inhibitors based on the structure of enzyme].
Jia, Hong; Guo, Yan-shen; Ge, Yi-yu; Wen, Hui; Yang, Jing; Yang, Xiu-ying; Du, Guan-hua; Yang, Guang-zhong.
Afiliação
  • Jia H; Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union'Medical College, Beijing 100050, China.
Yao Xue Xue Bao ; 42(12): 1271-81, 2007 Dec.
Article em Zh | MEDLINE | ID: mdl-18338640
A novel inhibitor series for matrix metalloproteinases (MMPs) were designed and synthesized. Using succinate and malonate as zinc binding groups and long hydrophobic substituents to bind with S1' pockets, the compounds showed micromolar inhibition and selectivity for MMP-2 over others. And we found a better activity compound. It is a chance to find a better precursor of MMP-2 inhibitors with activity and bioavailability by further optimization of compounds.
Assuntos
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Base de dados: MEDLINE Assunto principal: Desenho de Fármacos / Metaloproteinases da Matriz / Inibidores Enzimáticos / Inibidores de Metaloproteinases de Matriz Idioma: Zh Ano de publicação: 2007 Tipo de documento: Article
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Base de dados: MEDLINE Assunto principal: Desenho de Fármacos / Metaloproteinases da Matriz / Inibidores Enzimáticos / Inibidores de Metaloproteinases de Matriz Idioma: Zh Ano de publicação: 2007 Tipo de documento: Article