The synthesis and preliminary activity assay in vitro of peptide-like derivatives as APN inhibitors.
Both the aminopeptidase N (APN) and matrix metalloproteinase (MMP) are essential metallopeptidases in the development of tumor invasion and angiogenesis. A series of novel peptide-like derivatives were designed and synthesized as antitumor agents. Their structures were confirmed by IR, MS, and (1)H-NMR. These compounds exhibited potent inhibitory activities against APN and low activity against MMP in vitro. The derivatives with methoxy group show better activities than those with other substituted group and could be used as lead compounds for exploring new APN inhibitors in the future.
Li
Shao-hua
SH
State Key Laboratory of Food Science and Technology, Nanchang University, Nanchang 330047, PR China.
Li
Gang
G
Huang
Hui-ming
HM
Xiong
Fang
F
Liu
Cheng-mei
CM
Tu
Guo-gang
GG
D018826:CD13 Antigens / Q000037:antagonists & inhibitors*; D004926:Escherichia coli / Q000737:chemistry; D006860:Hydrogen Bonding; D013058:Mass Spectrometry; D061965:Matrix Metalloproteinase Inhibitors; D010455:Peptides / Q000138:chemical synthesis* / Q000494:pharmacology*; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D021241:Spectrometry, Mass, Electrospray Ionization; D013055:Spectrophotometry, Infrared
D061965:Matrix Metalloproteinase Inhibitors; D010455:Peptides; D011480:Protease Inhibitors; D018826:CD13 Antigens