Novel leucine ureido derivatives as inhibitors of aminopeptidase N (APN)

Chunhua Ma; Kang Jin; Jiangying Cao; Lei Zhang; Xiaoguang Li; Wenfang Xu

doi:10.1016/j.bmc.2013.01.068

Novel leucine ureido derivatives as inhibitors of aminopeptidase N (APN)

Bioorg Med Chem. 2013 Apr 1;21(7):1621-7. doi: 10.1016/j.bmc.2013.01.068. Epub 2013 Feb 9.

Authors

Chunhua Ma¹, Kang Jin, Jiangying Cao, Lei Zhang, Xiaoguang Li, Wenfang Xu

Affiliation

¹ Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University 44, West Culture Road, Jinan 250012, PR China.

PMID: 23453219
DOI: 10.1016/j.bmc.2013.01.068

Abstract

Aminopeptidase N (APN/CD13) over expressed on tumor cells, plays a critical role in tumor invasion, metastasis, and tumor angiogenesis. Here we described the design, synthesis and preliminary activity studies of novel leucine ureido derivatives as aminopeptidase N (APN/CD13) inhibitors. The results showed that compound 8c had the most potent inhibitory activity against APN with the IC50 value to 0.06 ± 0.041 μM, which could be used for further anticancer agent research.

Publication types

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

MeSH terms

Animals
Antineoplastic Agents / chemistry*
Antineoplastic Agents / pharmacology*
CD13 Antigens / antagonists & inhibitors*
CD13 Antigens / metabolism
Cell Line, Tumor
Drug Design
Humans
Inhibitory Concentration 50
Leucine / analogs & derivatives*
Leucine / pharmacology*
Molecular Docking Simulation
Neoplasms / drug therapy
Neoplasms / enzymology*
Protease Inhibitors / chemistry
Protease Inhibitors / pharmacology
Swine

Substances

Antineoplastic Agents
Protease Inhibitors
CD13 Antigens
Leucine