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

Bioorg Med Chem Lett

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

Published: November 2006

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.

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http://dx.doi.org/10.1016/j.bmcl.2006.07.059DOI Listing

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