Molecules | |
Investigation of the Biological Properties of (Hetero)Aromatic Thiosemicarbazones | |
Maciej Serda1  Anna Mrozek-Wilczkiewicz1  Josef Jampilek1  Matus Pesko1  Katarina Kralova1  Marcela Vejsova1  Robert Musiol1  Alicja Ratuszna1  | |
[1] 1Department of Organic Chemistry, Institute of Chemistry, University of Silesia, PL-40006 Katowice, Poland | |
关键词: thiosemicarbazones; lipophilicity; photosynthetic electron transport inhibition; spinach chloroplasts; iron chelators; in vitro antifungal activity; in vitro anticancer activity; | |
DOI : 10.3390/molecules171113483 | |
来源: mdpi | |
【 摘 要 】
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.
【 授权许可】
CC BY
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
【 预 览 】
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