Synthesis and biological evaluation of 20-epi-amino-20-deoxysalinomycin derivatives

Abstract

To improve the druggability of salinomycin, a 20-epi-amino-20-deoxysalinomycin derivatives library was synthesized with high efficacy from which a few salinomycin derivatives with high potency and selectivity were identified through comprehensive cytotoxicity assay, including a fluorine-19 magnetic resonance sensitive tool molecule. Using a K-ras cellular model, salinomycin and its derivatives showed different molecular mode of action from literature reports. These results would be valuable for developing salinomycin-based cancer therapy.

Keywords: (19)F MRI; Anti-cancer drugs; K-ras pathway; Nature product modification; Salinomycin; Staudinger reaction.