title: Novel matrix metalloproteinase inhibitors derived from quinoxalinone scaffold (Part I).
abstract: A series of quinoxalinone peptidomimetic derivatives was designed, synthesized, and assayed for their inhibitory activities on metalloproteinase-2 (MMP-2) and aminopeptidase N (APN). The results showed that all of these quinoxalinone derivatives displayed highly selective inhibition against MMP-2 as compared with APN, with IC(50) values in the micromole range. Compound A3 showed comparable MMP-2 inhibitory activities than the positive control LY52, which might be used as a potential lead in future research on anticancer agents.
authors.affiliation: School of Pharmaceutical Sciences, Shandong University, Ji'nan, 250012 Shandong Province, PR China.
authors.forename: Yonggang
authors.initials: Y
authors.lastname: Li
authors.forename: Jian
authors.initials: J
authors.lastname: Zhang
authors.forename: Wenfang
authors.initials: W
authors.lastname: Xu
authors.forename: Huawei
authors.initials: H
authors.lastname: Zhu
authors.forename: Xun
authors.initials: X
authors.lastname: Li
mesh_terms: D009682:Magnetic Resonance Spectroscopy; D061965:Matrix Metalloproteinase Inhibitors; D008958:Models, Molecular; D011480:Protease Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D011810:Quinoxalines / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D021241:Spectrometry, Mass, Electrospray Ionization; D013329:Structure-Activity Relationship
chemical_list: D061965:Matrix Metalloproteinase Inhibitors; D011480:Protease Inhibitors; D011810:Quinoxalines