Novel matrix metalloproteinase inhibitors derived from quinoxalinone scaffold (Part I).
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.
Li
Yonggang
Y
School of Pharmaceutical Sciences, Shandong University, Ji'nan, 250012 Shandong Province, PR China.
Zhang
Jian
J
Xu
Wenfang
W
Zhu
Huawei
H
Li
Xun
X
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
D061965:Matrix Metalloproteinase Inhibitors; D011480:Protease Inhibitors; D011810:Quinoxalines