Caffeine-hydrazones as anticancer agents with pronounced selectivity toward T-lymphoblastic leukaemia cells
Language English Country United States Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
25912310
DOI
10.1016/j.bioorg.2015.03.003
PII: S0045-2068(15)00021-8
Knihovny.cz E-resources
- Keywords
- Anticancer agents, Caffeine–hydrazones, Cancer treatment, Leukaemia, Selectivity,
- MeSH
- Precursor Cell Lymphoblastic Leukemia-Lymphoma drug therapy MeSH
- Anti-Infective Agents chemistry pharmacology MeSH
- Apoptosis drug effects MeSH
- Bacteria drug effects MeSH
- Cell Line MeSH
- Fungi drug effects MeSH
- Hydrazones chemistry pharmacology MeSH
- Caffeine chemistry pharmacology MeSH
- Humans MeSH
- Cell Line, Tumor MeSH
- Antineoplastic Agents chemistry pharmacology MeSH
- Structure-Activity Relationship MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Anti-Infective Agents MeSH
- Hydrazones MeSH
- Caffeine MeSH
- Antineoplastic Agents MeSH
We report design and synthesis of set of novel anticancer agents based on caffeine-hydrazones bearing 2-hydroxyaryl- or 2-N-heteroaryl moiety. Anticancer activity evaluation using seven cancer cell lines and two non-malignant cell lines demonstrated that several derivatives display significant anticancer activity and great selectivity index toward T-lymphoblastic leukaemia cells. In general, hydrazones bearing 2-N-heteroaryl moiety are more active and selective than those with 2-hydroxyaryl moiety. Tested compounds exhibit dose-dependent inhibition of both RNA and DNA synthesis, with some exceptions. Antimicrobial activities were tested on set of twelve bacterial and yeast strains, however prepared compounds were not active, suggesting for a molecular target specific for eukaryotic cells.
References provided by Crossref.org
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