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

Authors
Andrus, MB Turner, TM Updegraff, EP Sauna, ZE Ambudkar, SV
Citation
Mb. Andrus et al., Synthesis and analysis of polyethylene glycol linked P-glycoprotein-specific homodimers based on (-)-stipiamide, TETRAHEDR L, 42(23), 2001, pp. 3819-3822
Citations number
27
Categorie Soggetti
Chemistry & Analysis","Organic Chemistry/Polymer Science
Journal title
TETRAHEDRON LETTERS
ISSN journal
00404039 → ACNP
Volume
42
Issue
23
Year of publication
2001
Pages
3819 - 3822
Database
ISI
SICI code
0040-4039(20010604)42:23<3819:SAAOPG>2.0.ZU;2-N
Abstract
A series of five homodimeric polyethylene glycol (PEG) linked homodimers ba sed on the multidrug resistance reversal agent (-)-stipiamide were made and tested fur their ability to interact with P-glycoprotein, the protein resp onsible for multidrug resistance, using ATPase and photoaffinity displaceme nt assays. Key reactions include a new alkoxide-mesylate displacement for t he assembly of the PEG linkers and a double Sunogashira coupling reaction. (C) 2001 Elsevier Science Ltd. All rights reserved.