title: Inhibition of P-glycoprotein-mediated multidrug efflux by aminomethylene and ketomethylene analogs of reversins.
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.
authors.affiliation: Université Claude Bernard Lyon 1, Institut des Sciences Pharmaceutiques et Biologiques, EA 3741 Ecosystèmes et Molécules bioactives, 69373 Lyon cedex 08, France.
authors.forename: Ali
authors.initials: A
authors.lastname: Koubeissi
authors.forename: Imad
authors.initials: I
authors.lastname: Raad
authors.forename: Laurent
authors.initials: L
authors.lastname: Ettouati
authors.forename: David
authors.initials: D
authors.lastname: Guilet
authors.forename: Charles
authors.initials: C
authors.lastname: Dumontet
authors.forename: Joelle
authors.initials: J
authors.lastname: Paris
mesh_terms: 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*
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D009842:Oligopeptides; C120260:reversin 121