Synthesis and evaluation of cyclic nitrone derivatives as potential anti-cancer agents

Nitrones have been found to exhibit attractive biological values as immuno spin trapping agents. However, successful clinical cases of nitrone therapeutics are still lacking. Herein we report the synthesis and antiproliferative activity of a series of structurally diverse nitrone derivatives against a panel of 5 cancer cell lines, based on which indole- and pyrrole-fused were further evaluated by analogue preparation and in-vitro screening. Analogues with moderate to good potency were identified. This study shows the promise for further pursuit of nitrone-type small molecules in chemotherapy. [GRAPHICS] .

Automated summary

The synthesis and antiproliferative activity of a series of structurally diverse nitrone derivatives were reported, with indole- and pyrrole-fused analogues further evaluated through analogue preparation and in-vitro screening. Analogues with moderate to good potency were identified, showing promise for further pursuit of nitrone-type small molecules in chemotherapy.