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

M Roe; A Folkes; P Ashworth; J Brumwell; L Chima; S Hunjan; I Pretswell; W Dangerfield; H Ryder; P Charlton

doi:10.1016/s0960-894x(99)00030-x

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.

Authors

M Roe¹, A Folkes, P Ashworth, J Brumwell, L Chima, S Hunjan, I Pretswell, W Dangerfield, H Ryder, P Charlton

Affiliation

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.

MeSH terms

ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism*
Doxorubicin / pharmacology
Drug Resistance, Multiple*
Drug Synergism
Humans
Structure-Activity Relationship
Tumor Cells, Cultured
ortho-Aminobenzoates / chemistry
ortho-Aminobenzoates / pharmacology*

Substances

ATP Binding Cassette Transporter, Subfamily B, Member 1
ortho-Aminobenzoates
Doxorubicin
anthranilamide