Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 25, Issue 15, Pages 3005-3008Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2015.05.018
Keywords
1,4-Dihydroquinolines; P-gp inhibitor; Structure-activity relationships; Substrate properties; Mdr reversal
Categories
Funding
- DFG - Germany (German Research Foundation) [HI 687/6-3]
- European Union (EU) [1184256]
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Multidrug resistance (mdr) is the most important problem in the therapeutical treatment of cancer. One central problem in the resistance proceeding is the expression of transmembrane efflux pumps which transport drugs out of the cells. We developed novel substituted 1,4-dihydroquinolines as inhibitors of the transmembrane efflux pump P-glycoprotein. Structure-activity relationships are discussed for this first series. Promising active inhibitors have been identified and first bioanalytical studies have been carried out to address questions of cellular toxicity, P-gp substrate as well as mdr reversal properties. (C) 2015 Elsevier Ltd. All rights reserved.
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