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

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 IC50 values in micromole range. Compounds A1 and A2 showed comparable APN inhibitory activities than the positive control bestatin.

A series of novel l-iso-glutamine derivatives (A1–A18 and B1–B7) based on the antineoplaston AS2–5 scaffold were synthesized and evaluated for their in vitro enzymatic inhibitory activities against aminopeptidase N (APN, CD13) and MMP-2.Figure optionsDownload as PowerPoint slide