Design, synthesis, and preliminary studies of the activity of novel derivatives of N-cinnamoyl-L-aspartic acid as inhibitors of aminopeptidase N/CD13

Yingzi Liu; Luqing Shang; Hao Fang; Huawei Zhu; Jiajia Mu; Qiang Wang; Xuejian Wang; Yumei Yuan; Wenfang Xu

doi:10.1016/j.bmc.2009.07.014

Design, synthesis, and preliminary studies of the activity of novel derivatives of N-cinnamoyl-L-aspartic acid as inhibitors of aminopeptidase N/CD13

Bioorg Med Chem. 2009 Oct 15;17(20):7398-404. doi: 10.1016/j.bmc.2009.07.014. Epub 2009 Sep 24.

Authors

Yingzi Liu¹, Luqing Shang, Hao Fang, Huawei Zhu, Jiajia Mu, Qiang Wang, Xuejian Wang, Yumei Yuan, Wenfang Xu

Affiliation

¹ Department of Medicinal Chemistry, School of Pharmacy, Shandong University, 44 West Culture Road, 250012 Ji'nan, Shandong, PR China.

PMID: 19782572
DOI: 10.1016/j.bmc.2009.07.014

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Aspartic Acid / analogs & derivatives*
Aspartic Acid / pharmacology
CD13 Antigens / antagonists & inhibitors*
Cinnamates / pharmacology*
Drug Design*
HL-60 Cells
Humans
Magnetic Resonance Spectroscopy
Protease Inhibitors / chemistry*
Protease Inhibitors / pharmacology
Spectrometry, Mass, Electrospray Ionization

Substances

Cinnamates
Protease Inhibitors
Aspartic Acid
CD13 Antigens