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

Authors :: Serda M
Kalinowski DS
Mrozek-Wilczkiewicz A
Musiol R
Szurko A
Ratuszna A
Pantarat N
Kovacevic Z
Merlot AM
Richardson DR
Polanski J
Source :: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 Sep 01; Vol. 22 (17), pp. 5527-31. Date of Electronic Publication: 2012 Jul 15.
Publication Year :: 2012
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.<br /> (Copyright © 2012 Elsevier Ltd. All rights reserved.)

Subjects :: Antineoplastic Agents chemical synthesis
Cell Line, Tumor
Cell Proliferation drug effects
Deferoxamine pharmacology
Humans
Iron metabolism
Iron Chelating Agents chemical synthesis
Neoplasms drug therapy
Neoplasms metabolism
Quinolines chemical synthesis
Quinolines chemistry
Quinolines pharmacology
Thiosemicarbazones chemical synthesis
Antineoplastic Agents chemistry
Antineoplastic Agents pharmacology
Iron Chelating Agents chemistry
Iron Chelating Agents pharmacology
Thiosemicarbazones chemistry
Thiosemicarbazones pharmacology

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