Reversal of P-glycoprotein mediated multidrug resistance by novel anthranilamide derivatives

  • Bioorg Med Chem Lett. 1999 Feb 22;9(4):595-600. doi: 10.1016/s0960-894x(99)00030-x.
M Roe  1 ,  A Folkes ,  P Ashworth ,  J Brumwell ,  L Chima ,  S Hunjan ,  I Pretswell ,  W Dangerfield ,  H Ryder ,  P Charlton
Affiliations
  • 1. Xenova Ltd., Slough, England.
PMID: 10098671 DOI: 10.1016/s0960-894x(99)00030-x
Abstract

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.