A series of novel optically pure oxime esters derivatives were synthesized by the reaction of substitute keto oximes with various N-substituted α-amino acids chlorides in the presence of triethylamine and dichloromethane at 0°C, and their structures were characterized by IR, and 1D-NMR methods. The synthesized compounds were tested for their ability to inhibit the proliferation of human colon cancer cells and human epithelial cells. Some of them have been revealed a significant cytotoxic effect.