Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 117, Issue -, Pages 335-354Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2016.03.078
Keywords
Antitumor agents; Cancer; Chelators; Multidrug resistance; Schiff bases
Categories
Funding
- Hungarian Academy of Sciences
- ERC [StG-260572]
- NKTH-ANR [10-1-2011-0401]
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There is a constant need for new therapies against multidrug resistant (MDR) cancer. An attractive strategy is to develop chelators that display significant antitumor activity in multidrug resistant cancer cell lines overexpressing the drug efflux pump P-glycoprotein. In this study we used a panel of sensitive and MDR cancer cell lines to evaluate the toxicity of picolinylidene and salicylidene thiosemicarbazone, arylhydrazone, as well as picolinylidene and salicylidene hydrazino-benzothiazole derivatives. Our results confirm the collateral sensitivity of MDR cells to isatin-beta-thiosemicarbazones, and identify several chelator scaffolds with a potential to overcome multidrug resistance. Analysis of structure-activity relationships within the investigated compound library indicates that NNS and NNN donor chelators show superior toxicity as compared to ONS derivatives regardless of the resistance status of the cells. (C) 2016 Elsevier Masson SAS. All rights reserved.
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