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

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:16

Article

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

关键词: multidrug resistance;    P-glycoprotein;    reversin;    aminomethylene;    ketomethylene;    pseudopeptide;    chemosensitizer;   

DOI  :  10.1016/j.bmcl.2006.07.059

来源: Elsevier

【 摘 要 】

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. (c) 2006 Elsevier Ltd. All rights reserved.

【 授权许可】

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