Background: The present study emphasizes on designing a new series of isatin-dihydropyrimidinone
derivatives by adopting a hybrid pharmacophore approach. Fe3O4 nanoparticles (Fe3O4 NP) are magnetically recoverable and
are effective catalysts adequately used to synthesize Isatin-dihydropyrimidinones. Individual derivatives of Isatin and
dihydropyrimidinone are equipotent to treat cytotoxicity.
Objective: The present work was planned to fuse two pharmacophores (Isatin, dihydropyrimidinone) and to examine any
synergistic effect in the anticancer activity.
Method: The individual compounds are synthesized by adopting appropriate synthetic routes like sandmayers and
biginellis reaction and are fused together by using glacial acetic acid and Methanolic KOH to form novel Isatindihydropyrimidinone
hybrids. All the new series of hybrids 7a-l were characterized by FT-IR, 1
H NMR, 13
elemental analysis and Mass spectroscopy. The antioxidant activity of the synthesized compounds was assessed by using
two models: 1, 1-diphenyl-2-picryl-hydrazyl (DPPH) and Hydrogen peroxide (H2
) scavenging assay.
Results: From the results it can be inferred that nearly all the synthesized compounds have shown antioxidant activity
at the tested dose as correlated with the standard ascorbic acid. The in vitro cytotoxic activity was assayed by using
MTT assay. Compound 7l with IC50
values 22.13, 25.68 and 35.59 μM has significantly greater potency against MCF-
7, HeLa and IMR-32 cell lines.
Conclusion: The compounds with halogen and electron withdrawing groups at the C-5 position of isatin ring exhibited
significant antioxidant and cytotoxic activity.