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

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.