Novel aminopeptidase N inhibitors derived from antineoplaston AS2-5 (Part II)

Xun Li; Yazhou Wang; Jifeng Wu; Yonggang Li; Qiang Wang; Wenfang Xu

doi:10.1016/j.bmc.2009.03.017

Novel aminopeptidase N inhibitors derived from antineoplaston AS2-5 (Part II)

Bioorg Med Chem. 2009 Apr 15;17(8):3061-71. doi: 10.1016/j.bmc.2009.03.017. Epub 2009 Mar 14.

Authors

Xun Li¹, Yazhou Wang, Jifeng Wu, Yonggang Li, Qiang Wang, Wenfang Xu

Affiliation

¹ School of Pharmaceutical Sciences, Shandong University, No. 44 WenhuaXi Road, Ji'nan, 250012, Shandong Province, PR China.

PMID: 19339187
DOI: 10.1016/j.bmc.2009.03.017

Abstract

As our ongoing work, a series of peptidomimetic L-iso-glutamine derivatives derived from antineoplaston AS2-5 scaffold were prepared and their APN/CD13 and MMP-2 inhibitory activities were evaluated hereby. The results displayed that these compounds exhibited selective inhibition against APN as compared with MMP-2, with IC(50) values in micromole range. Compounds A1 and A2 showed comparable APN inhibitory activities than the positive control bestatin.

Publication types

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

MeSH terms

Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology
Binding Sites
CD13 Antigens / antagonists & inhibitors*
CD13 Antigens / chemistry
Glutamine / analogs & derivatives*
Glutamine / chemistry
Glutamine / pharmacology
Humans
Inhibitory Concentration 50
Models, Molecular
Phenylacetates / chemistry
Phenylacetates / pharmacology*
Protease Inhibitors / chemistry
Protease Inhibitors / pharmacology*
Structure-Activity Relationship

Substances

Antineoplastic Agents
Phenylacetates
Protease Inhibitors
Glutamine
CD13 Antigens