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Synthesis and biological evaluation of 2-benzoylpyridine thiosemicarbazones in a dimeric system: Structure-activity relationship studies on their anti-proliferative and iron chelation efficacy
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DOI：10.1016/j.jinorgbio.2014.07.020.png)
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Abstract
En 中文
Thiosemicarbazone chelators represent an exciting class of biologically active compounds that show great potential as anti-tumor agents. Our previous studies demonstrated the potent anti-tumor activity of the 2'-benzoylpyridine thiosemicarbazone series. While extensive studies have been performed on monomeric thiosemicarbazone compounds, dimeric thiosemicarbazone chelators have received comparatively less attention. Thus, it was of interest to investigate the anti-proliferative activity and iron chelation efficacy of dimeric thiosemicarbazones. Two classes of dimeric thiosemicarbazones were designed and synthesized. The first class consisted of two benzoylpyridine-based thiosemicarbazone units connected via a hexane or dodecane alkyl bridge, while the second class of dimer consisted of two thiosemicarbazones attached to a 2,6-dibenzoylpyridine core. These dimeric ligands demonstrated greater anti-proliferative activity than the clinically used iron chelator, desferrioxamine. This study highlights the importance of optimal lipophilicity as a factor influencing the cytotoxicity and iron chelation efficacy of these chelators. (C) 2014 Elsevier Inc. All rights reserved.
Keywords:
Thiosemicarbazone
Dimer
Lipophilicity
Iron
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