Synthesis and analysis of polyethylene glycol linked P-glycoprotein-specific homodimers based on (−)-stipiamide

…, TM Turner, EP Updegraff, ZE Sauna, SV Ambudkar

Index: Andrus, Merritt B.; Turner, Timothy M.; Updegraff, Emily P.; Sauna, Zuben E.; Ambudkar, Suresh V. Tetrahedron Letters, 2001 , vol. 42, # 23 p. 3819 - 3822

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Citation Number: 21

Abstract

A series of five homodimeric polyethylene glycol (PEG) linked homodimers based on the multidrug resistance reversal agent (−)-stipiamide were made and tested for their ability to interact with P-glycoprotein, the protein responsible for multidrug resistance, using ATPase and photoaffinity displacement assays. Key reactions include a new alkoxide-mesylate displacement for the assembly of the PEG linkers and a double Sonogashira coupling ...