Abstract
Polycyclic cage-like heterocyclic hybrids comprising structurally diverse heterocyclic units have been synthesized in good yields. Anticancer evaluation of these compounds against MCF-7 and NCI-H460 cell lines revealed dose dependent reduction with significant anticancer activity. Compound 4b inhibited these cell lines respectively with IC50 of 10.86 ± 0.94 and 9.17 ± 0.63 µM. Apoptosis and cell cycle analysis in MCF-7 revealed that this compound was able to induce early apoptosis.
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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 ± 0.63 µM 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.