Abstract A series of novel α-sulfonyl γ-(glycinyl-amino) proline peptidomimetic derivatives were designed, synthesized and assayed for their activities against matrix metalloproteinase- 2 (MMP-2), aminopeptidase N (APN)/CD13 and HDACs. The results indicated that all the compounds exhibited highly selective inhibition against MMP-2 as compared with APN and HDACs. The antiproliferative activities of some compounds against SKOV3, HL60 and ...