Synthesis and Evaluation of Novel Piperazine Hybrids as Promising Anticancer Agents
TL;DR
The results revealed that the synthesised derivative 3h has potential binding affinity hence blocking the activity, and the synthesised piperazine derivatives are identified as promising lead compounds for further anticancer optimization.
Abstract
This study aimed to synthesise a novel series of piperazine analogues (3a-k) having anticancer potential against MCF-7, MDA-MB-231 and HeLa cell lines. Structure of the synthesised analogues were confirmed through NMR and biological evaluation were done through MTT assay taking doxorubicin as a reference standard. The synthesised derivatives exhibited appreciable cytotoxicity at low concentrations. Molecular docking examined their binding interactions with estrogen receptor-α (ERα) and epidermal growth factor receptor (EGFR), associated with MCF-7 and MDA-MB-231 cell lines, respectively, providing structural insight into their anticancer potential. The results revealed that the synthesised derivative 3h has potential binding affinity hence blocking the activity. Therefore, the results obtained from in vitro and in silico studies identify the synthesised piperazine derivatives as promising lead compounds for further anticancer optimization. The IC50 values support this observation, with compounds 3g, 3h and 3i exhibiting the highest cytotoxic activity among the other derivatives evaluated.