Eco-friendly synthesis of novel enaminonitrile pyridine derivatives: 131I-radiosynthesis, anticancer investigation and in vivo study in tumour-bearing mice.

PURPOSE: This study aimed to develop sustainable synthetic routes for novel enaminonitrile pyridine derivatives and evaluate a lead compound's potential as a dual-action theranostic agent for oncology, combining targeted therapy and diagnostic imaging.

METHODS

Two green chemistry techniques were utilised: microwave-assisted and solvent-free mechanochemical grinding. The lead compound 7 was assessed for in vitro anticancer activity against MCF-7 cells. It was radiolabeled with iodine-131, optimising parameters like substrate amount and pH. Finally, in vivo biodistribution and tumour targeting were studied in tumour-bearing mice.

RESULTS

The green synthesis was highly efficient. Compound 7 showed superior anticancer activity (IC50 = 3.77 ± 0.43 µM) versus cisplatin. Radiolabeling achieved high radiochemical purity (95.74 ± 1.44%). Biodistribution studies confirmed excellent, selective tumour uptake (9.07% ID/g at 1 h) with sustained retention (7.91% ID/g at 24 h) and high target-to-background ratios.

CONCLUSIONS

This work successfully establishes efficient green synthesis routes. Compound 7 is a potent and selective sustainable theranostic agent, effectively merging green chemistry principles with precision oncology applications for both therapy and diagnosis.