Five ferrocenyl imidazo[1,2-a]pyridine compounds were synthesized by Groeb-ke-Blackburn-Bienaym? three-component-reaction (GBB-3CR) among 2-aminopyridine, ferro-cenecarboxaldehyde, and isocyanide with LaCl3 being catalyst in ethanol. The structure of the com-pounds were confirmed by proton magnetic resonance (1H NMR), carbon-13 magnetic resonance (13C NMR), and ultra high performance liquid chromatograph electrospray ion source mass spec-trometer (UHPLC-ESI-MS). Antioxidant abilities of the obtained compounds were evaluated by in-hibiting HO?- and Cu2 /glutathione (GSH)-induced oxidation of DNA. The radical-scavenging prop-erties of the obtained compounds were estimated by quenching 2,2?-azinobis(3-ethylbenzothiazoline-6-sulfonate) cationic radical (ABTS?) and 2,2?-diphenyl- 1-picrylhydrazyl (DPPH?), and then the effects of substituents on the antioxidant properties of fer-rocenyl imidazo[1,2-a]pyridine compounds could be explored. The results showed that the TBARS percentages of five compounds were 65.4%~93.7% in inhibiting HO?- induced oxidation of DNA. The TBARS percentages of five compounds were 25.6%~62.5% in inhibiting GS?- induced oxidation of DNA. All five ferrocenyl imidazo[1,2-a]pyridine compounds could scavenge ABTS? and DPPH?. The compounds VI containing two ferrocenyls exhibits higher activity than other compounds in quenching radicals and inhibiting radicals induced oxidation of DNA.