Reversal of P-Glycoprotein Mediated Multidrug Resistance by Novel Anthranilamide Derivatives.

We have synthesised and evaluated a series of anthranilamide based modulators of P-glycoprotein. These studies have identified XR9576(2), a potent inhibitor of P-glycoprotein in vitro and in vivo. The general synthesis and the SAR of these compounds are described.