Synthesis and structure–activity relationships of sinenxan A derivatives as multidrug resistance reversal agents

Two types of sinenxan A derivatives with different side chains at C-5 were synthesized and evaluated for their in vitro multidrug resistant reversal activities. Several derivatives exhibited better activities than the positive control verapamil. The structure–activity relationships of these derivatives suggested that a carbonyl group at C-13 and the length of side chain at C-5 are important for the activity.

Graphical abstractA series of new taxoids derived from sinenxan A were synthesized and evaluated for their in vitro multidrug resistant reversal activities. Four derivatives exhibited better activities than the positive control verapamil. Structure–activity relationships of these derivatives were explored as well.Figure optionsDownload full-size imageDownload as PowerPoint slide