Synthesis and analysis of polyethylene glycol linked P-glycoprotein-specific homodimers based on (−)-stipiamide
作者:Merritt B Andrus、Timothy M Turner、Emily P Updegraff、Zuben E Sauna、Suresh V Ambudkar
DOI:10.1016/s0040-4039(01)00619-0
日期:2001.6
A series of five homodimeric polyethylene glycol (PEG) linked homodimers based on the multidrug resistance reversal agent (-)-stipiamide were made and tested fur 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 Sunogashira coupling reaction. (C) 2001 Elsevier Science Ltd. All rights reserved.