Abstract
A Series of hybrid organic nitrogen compounds 4, 6, and 8 were synthesized and confirmed through the use of different spectroscopic techniques (IR, NMR, and MS spectrometry) along with elemental analysis. The in vitro antitumor activity of the compounds (4b–d), (6b,c), and (8b,c) against A549 and MCF-7 cell lines and normal breast and lung cells were assessed. Several compounds were found to be potent antitumor agents. Further, in vitro cell cycle study of compounds, 4d and 8c revealed A549 and MCF-7 cell cycle arrest at S and G2/ M phases, respectively; and induce apoptosis at the pre-G1 phase. The apoptosis-inducing activity of synthesized compounds was proofed by the elevation of caspase 3/7 activity and also by up-regulation of the expression of Bax and p53 proteins together with the down-regulation of the expression of the Bcl-2 protein. They also had a strong inhibitory effect against β-tubulin polymerization and topoisomerase IIβ enzyme.
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