Progesterone–adenine hybrids as bivalent inhibitors of P-glycoprotein-mediated multidrug efflux: Design, synthesis, characterization and biological evaluation
…, S Radix, T Lomberget, A Dumoulin, R Barret, C Grenot…
Index: Zeinyeh, Wael; Mahiout, Zahia; Radix, Sylvie; Lomberget, Thierry; Dumoulin, Axel; Barret, Roland; Grenot, Catherine; Rocheblave, Luc; Walchshofer, Nadia; Matera, Eva-Laure; Dumontet, Charles Steroids, 2012 , vol. 77, # 12 p. 1177 - 1191,15 Title/Abstract Full Text Show Details Zeinyeh, Wael; Mahiout, Zahia; Radix, Sylvie; Lomberget, Thierry; Dumoulin, Axel; Barret, Roland; Grenot, Catherine; Rocheblave, Luc; Matera, Eva-Laure; Dumontet, Charles; Walchshofer, Nadia Steroids, 2012 , vol. 77, # 12 p. 1177 - 1191
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Citation Number: 6
Abstract
Bivalent ligands were designed on the basis of the described close proximity of the ATP-site and the putative steroid-binding site of P-glycoprotein (ABCB1). The syntheses of 19 progesterone–adenine hybrids are described. Their abilities to inhibit P-glycoprotein- mediated daunorubicin efflux in K562/R7 human leukemic cells overexpressing P- glycoprotein were evaluated versus progesterone. The hybrid with a hexamethylene linker ...