title: Fe3O4 Nanoparticles Mediated Synthesis of Novel Isatin-dihydropyrimidinone Hybrid Molecules as Antioxidant and Cytotoxic Agents.
abstract: 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.
  
  
  METHODS
  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, 1H NMR, 13C NMR, 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 (H2O2) 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.
  
  
  CONCLUSIONS
  The compounds with halogen and electron withdrawing groups at the C-5 position of isatin ring exhibited significant antioxidant and cytotoxic activity.
authors.affiliation: Centre for Pharmaceutical Sciences, Institute of Science and Technology, Jawaharlal Nehru Technological University Hyderabad, Kukatpally-500085, India.
authors.forename: Srinubabu
authors.initials: S
authors.lastname: Maddela
authors.affiliation: Centre for Pharmaceutical Sciences, Institute of Science and Technology, Jawaharlal Nehru Technological University Hyderabad, Kukatpally-500085, India.
authors.forename: Ajitha
authors.initials: A
authors.lastname: Makula
authors.affiliation: Centre for nanoscience and technology, Institute of Science and Technology, Jawaharlal Nehru Technological University Hyderabad, Kukatpally-500085, India.
authors.forename: N
authors.initials: N
authors.lastname: Jayarambabu
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000975:Antioxidants / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D052203:Ferrosoferric Oxide / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D007510:Isatin / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D011744:Pyrimidinones / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D000975:Antioxidants; D011744:Pyrimidinones; D007510:Isatin; D052203:Ferrosoferric Oxide
keywords: Cytotoxicity; DPPH; Fe3O4 NP; H2O2 Scavenging assay; Isatin-dihydropyrimidinone hybrids