In Vitro cytotoxicity and antioxidant evaluation of 7-amino-2-styrylchromone derivatives

Objective: The objective of this study was to synthesize 7-amino-2-styrylchromone derivatives and evaluate their in vitro cytotoxic and antioxidant potential. Methods: 7-amino-2-styrylchromones were synthesized from 7-amino-2-methylchromone by condensing it with various substituted aromatic aldehydes. The cytotoxicity of the synthesized molecules was assessed against two cell lines, MCF-7 and HCT-116 by 3-(4,5-dimethyl thiazol-2-yl)-2,5- diphenyl tetrazolium bromide assay. Cell cycle analysis of the most potent molecule ASC-7 was carried out. The antioxidant studies were conducted by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and nitric oxide methods. Result: (E)-7-amino-2-(3,4-methylenedioxystyryl)-4H-chromen-4-one (ASC-7) with inhibitory concentration 50% (IC₅₀) 56.0 µM was found to be the most potent molecule against MCF-7. ASC-7 induced G₀/G₁ phase arrest of MCF-7. Furthermore, (E)-7-amino-2-(3,4-methylenedioxystyryl)- 4H-chromen-4-one(ASC-7) showed good DPPH scavenging activity (IC₅₀ 54.6 µM). However, none of the tested compounds exhibited nitric oxide scavenging property. Conclusion: This study reports the synthesis of 7-amino-2-styrylchromones. Some of the synthesized compounds showed moderate cytotoxicity against the tested cell lines MCF-7 and HCT-116. (E)-7-amino-2-(3,4-methylenedioxystyryl)-4H-chromen-4-one (ASC-7) was found to be the best cytotoxic and antioxidant agent.