Design, synthesis and evaluation of progesterone-adenine hybrids as bivalent inhibitors of P-glycoprotein-mediated multidrug efflux

作者：Zeinyeh Wael; Alameh Ghina; Radix Sylvie^*; Grenot Catherine; Dumontet Charles; Walchshofer Nadia

来源：Bioorganic & Medicinal Chemistry Letters, 2010, 20(10): 3165-3168.

DOI：10.1016/j.bmcl.2010.03.085

• Multidrug resistance
• P-Glycoprotein
• ABCB1
• Bivalent ligand
• Multivalent ligand
• Progesterone
• Adenine

Steroidal bivalent ligands were designed on the basis of the described closer proximity of the ATP-site and the putative steroid-binding site of P-glycoprotein (ABCB1). The syntheses of seven progesterone-adenine hybrids were described. Their abilities to inhibit P-glycoprotein-mediated daunorubicin efflux in K562/R7 human leukemic cells overexpressing P-glycoprotein were evaluated versus progesterone.

• 出版日期2010-5-15