Facilely accessible multidrug resistance modulator derived from sucrose

Exploration for new MDR-modulators utilizing atractysucroses as scaffolds disclosed 2,3,4,3′,4′-O-pentaisovalerylsucrose (9) as a readily accessible medicinal lead. This lead was prepared from sucrose in 65% total yield for three steps. In addition, compound 9 exhibited more potent MDR modulating activity than verapamil, a representative modulator of MDR mediated by P-gp.