SYNTHESIS, CHARACTERIZATION AND ANTICANCER ACTIVITY OF PIPERAZINE AMIDE DERIVATIVEAbstract
Piperazine is a nitrogen-containing heterocyclic compound and has fascinating applications in drug discovery and development. In the present study, novel 4-(benzo[1,3]dioxol-5-ylmethyl) piperazine amide derivative was prepared by acid amine coupling of 1-piperonyl piperazine derivative and benzoic acid. Synthesized compound was characterized by IR, NMR and mass spectral studies. Further, in-vitro cytotoxic effects were carried out in MTT in various human cell lines HeLa, MCF7, MDA-MB-231, HCT116, and HT29. Out of these diverse cell lines, compound 3 showed promising cytotoxic effects on MDA-MB-231 with the IC50 estimation of 11.3 µM. The surface morphology by Colonogenic assay and in-vitro cell migration assay measures better movement on MDA-MB-231 in compound 3. Further, apoptotic-related examination under AO/Eb staining, commet assay, and cell cycle investigation exhibited that compound 3 demonstrated significant activities on MDA-MB-231 by activates apoptosis and blocking cell cycle moment in the G0/G1 stage. All the more altogether, staining the cells in the meantime with Annexin V-FITC/PI. The synthesized compound 3 indicated tremens-dous repressing capacities in cell cycle and activates apoptosis because of the structural morphology and heteroatom present in the molecule.
B. K. Sagar *, M. Dileep Kumar, Mahesh Bhat, E. Vijaya Sekhar and M. Supreeth
Department of Chemistry, MDRPU Science College, Varakodu, Mysore, Karnataka, India.
23 October 2020
15 February 2021
24 May 2021
01 October 2021