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Abstract With an aim to construct novel anticancer drugs, a series of polycyclic heterocycles comprising diverse structural sub-units based on molecular hybridization strategy have been designed and synthesized through a… Click to show full abstract
Abstract With an aim to construct novel anticancer drugs, a series of polycyclic heterocycles comprising diverse structural sub-units based on molecular hybridization strategy have been designed and synthesized through a three-component [3+2]-cycloaddition/annulation strategy. Anticancer evaluation of these compounds against MCF-7 and NCI-H460 cell lines revealed dose dependent reduction with noteworthy anticancer activity. Compound 4b inhibited MCF-7 and NCI-H460 cell lines with IC50 values 10.86±0.94 and 9.17±0.63µM respectively. Further, apoptosis and cell cycle analysis revealed that this compound was able to prompt apoptosis at an early stage in MCF-7 cell line besides increasing the threshold of MMP and % of cells expressing FITC-dUTP. These results suggest that compound 4b is a potential molecule for the further exploration.
Journal Title: Journal of King Saud University - Science
Year Published: 2021
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