Inhibition of P-glycoprotein-mediated multidrug efflux by aminomethylene and ketomethylene analogs of reversins

Ali Koubeissi; Imad Raad; Laurent Ettouati; David Guilet; Charles Dumontet; Joelle Paris

doi:10.1016/j.bmcl.2006.07.059

Inhibition of P-glycoprotein-mediated multidrug efflux by aminomethylene and ketomethylene analogs of reversins

Bioorg Med Chem Lett. 2006 Nov 1;16(21):5700-3. doi: 10.1016/j.bmcl.2006.07.059. Epub 2006 Sep 6.

Authors

Ali Koubeissi¹, Imad Raad, Laurent Ettouati, David Guilet, Charles Dumontet, Joelle Paris

Affiliation

¹ Université Claude Bernard Lyon 1, Institut des Sciences Pharmaceutiques et Biologiques, EA 3741 Ecosystèmes et Molécules bioactives, 69373 Lyon cedex 08, France.

PMID: 16950619
DOI: 10.1016/j.bmcl.2006.07.059

Abstract

Several aminomethylene analogs and a ketomethylene analog of reversins were synthesized in order to evaluate their ability to inhibit P-glycoprotein-mediated drug efflux in K562/R7 human leukemic cells overexpressing P-glycoprotein. These analogs retained good activity compared to cyclosporin A and the original reversins.

MeSH terms

ATP Binding Cassette Transporter, Subfamily B, Member 1 / antagonists & inhibitors*
Drug Resistance, Multiple / drug effects*
Humans
K562 Cells
Oligopeptides / pharmacology*

Substances

ATP Binding Cassette Transporter, Subfamily B, Member 1
Oligopeptides
reversin 121