• Bioorg. Med. Chem. Lett. · Feb 2013

    Synthesis and biological evaluation of substituted 2-benzoylpyridine thiosemicarbazones: novel structure-activity relationships underpinning their anti-proliferative and chelation efficacy.

    • Adeline Y Lukmantara, Danuta S Kalinowski, Naresh Kumar, and Des R Richardson.
    • School of Chemistry, University of New South Wales, Sydney, NSW 2052, Australia.
    • Bioorg. Med. Chem. Lett. 2013 Feb 15; 23 (4): 967-74.

    AbstractThe 2-benzoylpyridine thiosemicarbazone (BpT) chelators demonstrate potent anti-proliferative effects against tumor cells. To understand their structure-activity relationships, BpT analogues incorporating electron-donating substituents on the pyridine and phenyl rings of the BpT scaffold were designed and represent the first attempts to modify the pyridine ring of these thiosemicarbazones. Eight analogues showed significantly (p <0.001) greater anti-proliferative activity than the 'gold-standard' chelator, desferrioxamine. Structure-activity analysis revealed that mono- or di-methoxy substitution at the phenyl ring resulted in lower anti-proliferative activity, while methoxy substitutions at the phenyl ring enhanced iron chelation efficacy. These important findings facilitate the design of thiosemicarbazones with greater anti-tumor activity.Copyright © 2012 Elsevier Ltd. All rights reserved.

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