Smallest peptoids with antiproliferative activity on human neoplastic cells.

Libraries of new, small peptoid monomers and dipeptoids were synthesized and assayed for antiproliferative activity against representative human neoplastic cell lines. The C-terminal N-alkyl amide peptoids are cytotoxic and are the smallest peptoids reported to have such activity. These compounds were conveniently synthesized on a BAL resin. Owing to their structure, the peptoids did not suffer from DKP formation, a problematic side reaction typically observed in peptide and peptoid synthesis.