DESIGN, SYNTHESIS amp; AMINO ACID COMPOSITION OF FULLERENE BASED PEPTIDOMIMETICS AGAINST LEUKEMIA AND OVERIAN CANCER

摘要

The objective of the present study describes an approach to synthesize smaller chain peptides by liquid phase peptide synthesis and to test for in vitro anticancer activity on leukemia and ovarian cell lines. Based on rational drug design using Lipinski rule, Boman index and HDAC docking, 4 peptide scaffolds were selected and synthesized, viz., Peptidomimetics 1, 2, 3 and 4 [Fullerene C60-Arg-Lys (RK), Fullerene C60-Lys-Hist. (KH), Fullerene C60-Arg-Arg-Hist. (RRH) and Fullerene C60- Arg-Arg-T,ys. (RRK)]. All the synthesized compounds were purified by column chromatography and further confirmed by Melting point, IR and Mass spectral data. The anticancer activity of different concentrations of the test drugs was determined using MTT assay and IC50 values of the test compounds were subsequently compared with that of standard drug. Peptidomimetics test drug 4 have shown maximum anticancer activity against leukemia cell line with IC50 value 8 |ig/mL whereas test drug 2 have shown maximum activity against ovarian cancer cell line with IC50 value 7.1 |ig/mL which clearly indicates that these peptidomimetics are potent anticancer agents for leukemia and ovarian cancer cell lines.