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

Ali Koubeissi (1) , Imad Raad (1) , Laurent Ettouati (1) , David Guilet (1) , Charles Dumontet (2) , Joëlle Paris (1)

1 Ecosystèmes et Molécules Bioactives
2 Oncogénèse et progression tumorale

— 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.

Domaines: Médicaments; Chimie thérapeutique

Ali Koubeissi, Imad Raad, Laurent Ettouati, David Guilet, Charles Dumontet, et al.. Inhibition of P-glycoprotein-mediated multidrug efflux by aminomethylene and ketomethylene analogs of reversins. Bioorganic and Medicinal Chemistry Letters, 2006, 16 (21), pp.5700 - 5703. ⟨10.1016/j.bmcl.2006.07.059⟩. ⟨hal-01653673⟩