title: [Design, synthesis and activity evaluation of novel matrix metalloproteinases inhibitors based on the structure of enzyme].
abstract: 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.
authors.affiliation: Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union'Medical College, Beijing 100050, China.
authors.forename: Hong
authors.initials: H
authors.lastname: Jia
authors.forename: Yan-shen
authors.initials: YS
authors.lastname: Guo
authors.forename: Yi-yu
authors.initials: YY
authors.lastname: Ge
authors.forename: Hui
authors.initials: H
authors.lastname: Wen
authors.forename: Jing
authors.initials: J
authors.lastname: Yang
authors.forename: Xiu-ying
authors.initials: XY
authors.lastname: Yang
authors.forename: Guan-hua
authors.initials: GH
authors.lastname: Du
authors.forename: Guang-zhong
authors.initials: GZ
authors.lastname: Yang
mesh_terms: D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry; D061965:Matrix Metalloproteinase Inhibitors; D020782:Matrix Metalloproteinases / Q000138:chemical synthesis* / Q000737:chemistry; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D061965:Matrix Metalloproteinase Inhibitors; D020782:Matrix Metalloproteinases