Design, synthesis, and preliminary studies of the activity of novel derivatives of N-cinnamoyl-L-aspartic acid as inhibitors of aminopeptidase N/CD13.
A series of novel derivatives of N-cinnamoyl-l-aspartic acid were designed, synthesized, and assayed for their inhibitory activities against aminopeptidase N. The preliminary biological assay showed that compound 8c has the most potent inhibitory activity against APN with an IC(50) of 11.1+/-0.9 microM, this could be used as the lead compound in future research on anticancer agents.
Department of Medicinal Chemistry, School of Pharmacy, Shandong University, 44 West Culture Road, 250012 Ji'nan, Shandong, PR China.
Yingzi
Y
Liu
Luqing
L
Shang
Hao
H
Fang
Huawei
H
Zhu
Jiajia
J
Mu
Qiang
Q
Wang
Xuejian
X
Wang
Yumei
Y
Yuan
Wenfang
W
Xu
D001224:Aspartic Acid / Q000031:analogs & derivatives* / Q000494:pharmacology; D018826:CD13 Antigens / Q000037:antagonists & inhibitors*; D002934:Cinnamates / Q000494:pharmacology*; D015195:Drug Design; D018922:HL-60 Cells; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D011480:Protease Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D021241:Spectrometry, Mass, Electrospray Ionization
D002934:Cinnamates; D011480:Protease Inhibitors; D001224:Aspartic Acid; D018826:CD13 Antigens