Inhibition of P-glycoprotein-mediated multidrug efflux by aminomethylene and ketomethylene analogs of reversins.
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.
Koubeissi
Ali
A
Université Claude Bernard Lyon 1, Institut des Sciences Pharmaceutiques et Biologiques, EA 3741 Ecosystèmes et Molécules bioactives, 69373 Lyon cedex 08, France.
Raad
Imad
I
Ettouati
Laurent
L
Guilet
David
D
Dumontet
Charles
C
Paris
Joelle
J
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000037:antagonists & inhibitors*; D018432:Drug Resistance, Multiple / Q000187:drug effects*; D006801:Humans; D020014:K562 Cells; D009842:Oligopeptides / Q000494:pharmacology*
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D009842:Oligopeptides; C120260:reversin 121