Novel 3-phenylpropane-1,2-diamine derivates as inhibitors of aminopeptidase N (APN)

Luqing Shang; Qiang Wang; Hao Fang; Jiajia Mu; Xuejian Wang; Yumei Yuan; Binghe Wang; Wenfang Xu

doi:10.1016/j.bmc.2008.10.025

Novel 3-phenylpropane-1,2-diamine derivates as inhibitors of aminopeptidase N (APN)

Bioorg Med Chem. 2008 Dec 1;16(23):9984-90. doi: 10.1016/j.bmc.2008.10.025. Epub 2008 Oct 14.

Authors

Luqing Shang¹, Qiang Wang, Hao Fang, Jiajia Mu, Xuejian Wang, Yumei Yuan, Binghe Wang, Wenfang Xu

Affiliation

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

PMID: 18996018
DOI: 10.1016/j.bmc.2008.10.025

Abstract

Aminopeptidase N (APN) is an essential peptidase involved in the process of tumor invasion and metastasis. Here we describe a novel class of inhibitor with 3-phenylpropane-1,2-diamine as scaffold to APN. Preliminary activity evaluation with enzyme inhibition studies showed that compound 12i exhibited potent and selective inhibitory activity towards APN with the IC(50) value 15.5+/-1.2microM.

Publication types

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

MeSH terms

CD13 Antigens / antagonists & inhibitors*
CD13 Antigens / chemistry
CD13 Antigens / pharmacology
Cells, Cultured
Diamines / chemical synthesis
Diamines / chemistry
Diamines / pharmacology*
HL-60 Cells
Humans
Inhibitory Concentration 50
Matrix Metalloproteinase 2 / pharmacology
Matrix Metalloproteinase Inhibitors
Microsomes / drug effects
Microsomes / metabolism
Protease Inhibitors / chemical synthesis
Protease Inhibitors / chemistry
Protease Inhibitors / pharmacology*
Structure-Activity Relationship

Substances

Diamines
Matrix Metalloproteinase Inhibitors
Protease Inhibitors
CD13 Antigens
Matrix Metalloproteinase 2