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Investigation of the biological properties of (hetero)aromatic thiosemicarbazones.

Authors
  • Serda, Maciej
  • Mrozek-Wilczkiewicz, Anna
  • Jampilek, Josef
  • Pesko, Matus
  • Kralova, Katarina
  • Vejsova, Marcela
  • Musiol, Robert
  • Ratuszna, Alicja
  • Polanski, Jaroslaw
Type
Published Article
Journal
Molecules
Publisher
MDPI AG
Publication Date
Jan 01, 2012
Volume
17
Issue
11
Pages
13483–13502
Identifiers
DOI: 10.3390/molecules171113483
PMID: 23151918
Source
Medline
License
Unknown

Abstract

Two series of thiosemicarbazone-based iron chelators (twenty-seven compounds) were designed and synthesized using a microwave-assisted approach. Quinoline and halogenated phenyl were selected as parent scaffolds on the basis of a similarity search. The lipophilicity of the synthesized compounds was measured using HPLC and then calculated. Primary in vitro screening of the synthesized compounds was performed against eight pathogenic fungal strains. Only a few compounds showed moderate activity against fungi, and (E)-2-(quinolin-2-ylvinyl)-N,N-dimethylhydrazine-carbothioamide appeared to be more effective than fluconazole against most of the fungal strains tested. Antiproliferative activity was measured using a human colon cancer cell line (HCT-116). Several of the tested compounds showed submicromolar antiproliferative activity. Compounds were also tested for their activity related to the inhibition of photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. The structure-activity relationships are discussed for all of the compounds.

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