Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 84, Issue -, Pages 173-180Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.07.003
Keywords
Chalcones; Flavanones; Flavones; Cytotoxic; Leukemia; Anti-inflammatory
Categories
Funding
- Fundacao para a Ciencia e a Tecnologia (FCT, Portugal)
- European Union
- QREN
- FEDER [PEst-C/QUI/UI0062/2013, FCOMP-01-0124-FEDER-037296]
- COMPETE
- Portuguese National NMR Network
- Recherche Cancer et Sang foundation
- Recherches Scientifiques Luxembourg asbl
- Een Haerz fir Kriibskrank Kanner association
- Action Lions Vaincre le Cancer Luxembourg
- National Research Foundation (NRF) by the MEST of Korea for Tumor Microenvironment Global Core Research Center (GCRC) grant [2012-0001184]
- Seoul National University Research grant
- Research Settlement Fund for the new faculty of SNU
- Research Institute of Pharmaceutical Sciences
Ask authors/readers for more resources
A new series of chalcones, flavanones and flavones with methylenedioxy group at the 3',4' position in chalcone, 7,8 position in flavanones and flavones with mono-, di- and trimethoxy groups in the benzaldehyde ring have been assessed for their effect on proliferation, cytotoxic potential and apoptosis in human leukemia cells. Among the tested compounds, the chalcone series showed the best activity and chalcone 3 (mono methoxy group at the ortho position in A-ring) showed a significant effect on downregulation of cancer cell proliferation and viability in three different leukemia cell lines (K562, Jurkat, U937). The executioner caspase cleavage analyses indicated that the cytotoxic effect mediated by chalcone 3 is due to induction of apoptotic cell death. Interestingly, the cytotoxic effect was cell type-specific and targeted preferentially cancer cells as peripheral blood mononuclear cells (PBMCs) from healthy donors were less affected by the treatment compared to K562, Jurkat and U937 leukemia cells. Altogether our results indicate a potential drug candidate with interesting differential toxicity obeying Lipinski's rule of five. (c) 2014 Elsevier Masson SAS. All rights reserved.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available