Design, synthesis and biological evaluation of thiosemicarbazones, hydrazinobenzothiazoles and arylhydrazones as anticancer agents with a potential to overcome multidrug resistance

Veronika F.S. Pape, Szilárd Tóth, András Füredi, Kornélia Szebényi, Anna Lovrics, Pál Szabó, Michael Wiese, Gergely Szakács

Research output: Article

36 Citations (Scopus)


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.

Original languageEnglish
Pages (from-to)335-354
Number of pages20
JournalEuropean Journal of Medicinal Chemistry
Publication statusPublished - júl. 19 2016


ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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