2. Academic Validation
  3. Synthesis and characterization of quinoline-based thiosemicarbazones and correlation of cellular iron-binding efficacy to anti-tumor efficacy

Synthesis and characterization of quinoline-based thiosemicarbazones and correlation of cellular iron-binding efficacy to anti-tumor efficacy

  • Bioorg Med Chem Lett. 2012 Sep 1;22(17):5527-31. doi: 10.1016/j.bmcl.2012.07.030.
Maciej Serda 1,  Danuta S Kalinowski,  Anna Mrozek-Wilczkiewicz,  Robert Musiol,  Agnieszka Szurko,  Alicja Ratuszna,  Namfon Pantarat,  Zaklina Kovacevic,  Angelica M Merlot,  Des R Richardson,  Jaroslaw Polanski
Affiliations

Affiliation

  • 1 Department of Organic Chemistry, Institute of Chemistry, University of Silesia, PL-40006 Katowice, Poland.
PMID: 22858101 DOI: 10.1016/j.bmcl.2012.07.030
Abstract

Iron chelators have emerged as a potential anti-cancer treatment strategy. In this study, a series of novel thiosemicarbazone iron chelators containing a quinoline scaffold were synthesized and characterized. A number of analogs show markedly greater anti-cancer activity than the 'gold-standard' iron chelator, desferrioxamine. The anti-proliferative activity and iron chelation efficacy of several of these ligands (especially compound 1b), indicates that further investigation of this class of thiosemicarbazones is worthwhile.

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