Because of the medicinal application of peptides in the current drug discovery process, we report the
synthesis and in vitro anticancer activity of various pregabalin containing peptides using chiral amino
acids. The structures of newly synthesized compounds were assigned based on IR, 1H NMR, 13C
NMR and mass spectral analysis. Synthesized peptides were screened for their anticancer activity on
human breast cancer MCF-7 cells line by MMT assays method. Evaluation of anticancer activity
shown that compound 13a (16.65% cell proliferation) was found to be most active against selected
MCF-7 cell line.