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.
Aims: Herein, we report the cytotoxicity of gabapentin-based peptides (11a-11j) using L-alanine and L-phenyl alanine chiral amino acids for peptide bond formation in ten efficient and straightforward steps. The in vitro MTT assays of derived molecules on the MCF-7 cell line (a human breast adenocarcinoma cell line) exhibited enhanced antitumor activity compared to the control (100% cell proliferation).
Methods: The ten steps synthetic methods were adapted for the synthesis of the Gabapentin-based peptide derivatives through BOC- deBOC methods and using EDC-HCl, DMAP and commercially available solvents. All the synthesized peptides were unambiguously characterized with the help of spectroscopic (IR, 1H NMR, 13C-NMR, mass spectra, and elemental) data analysis.
Results: The Compounds 11a, 11b, 11h,11i, and 11j showed a remarkable antiproliferative (cell death) activity, with % cell proliferation values ranging from 25-38 %.
Conclusion: The study showed that the compounds with some specific functionalities like, benzylic and trifluoromethyl functionality enhanced the potency with comparable %cell proliferation and cell death. Based on the findings in this work and their easily accessible molecular structures, compounds 11a and 11j are worthy of further biological investigations.
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