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Design, synthesis and biological evaluation of thiosemicarbazones, hydrazinobenzothiazoles and arylhydrazones as anticancer agents with a potential to overcome multidrug resistance.
- Source :
-
European journal of medicinal chemistry [Eur J Med Chem] 2016 Jul 19; Vol. 117, pp. 335-54. Date of Electronic Publication: 2016 Mar 30. - Publication Year :
- 2016
-
Abstract
- 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-β-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.<br /> (Copyright © 2016 Elsevier Masson SAS. All rights reserved.)
- Subjects :
- Antineoplastic Agents chemistry
Antineoplastic Agents pharmacology
Benzothiazoles chemistry
Cell Line, Tumor
Drug Resistance, Multiple drug effects
Drug Resistance, Neoplasm drug effects
Humans
Hydrazones chemistry
Structure-Activity Relationship
Thiosemicarbazones chemistry
Benzothiazoles pharmacology
Hydrazones pharmacology
Thiosemicarbazones pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1768-3254
- Volume :
- 117
- Database :
- MEDLINE
- Journal :
- European journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 27161177
- Full Text :
- https://doi.org/10.1016/j.ejmech.2016.03.078