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The present review covers the recent synthetic amino acid derivatives and chemical transformations to peptide derivatives with anticancer and antimicrobial activity. Amino acid derivatives are an import group of peptidomimetics with a variety of applications in medicinal chemistry. This derivatives possess several biological activities such as anti-microbial anti-tumor effect and DNA binding activity. Moreover, most natural peptides are widely prevalence and composed of amino acids, and limited bio-stability, and low bio-availability. To overcome this problems, the biologically active pseudo-peptides have been developed, which have highly specificity and non-toxicity pharmaceuticals. The present work show synthesis small molecules contaning amino acids with antimicrobial and anticancer activities and DNA binding activity.