Mathieu 2013 J Med Chem: Difference between revisions
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|journal=J Med Chem | |journal=J Med Chem | ||
|abstract=We designed and synthesized 48 aryl-1H-imidazole derivatives and investigated their ''in vitro'' growth inhibitory activity in cancer cell lines known to present various levels of resistance to proapoptotic stimuli. The IC50 ''in vitro'' growth inhibitory concentration of these compounds ranged from >100 ΞΌM to single digit ΞΌM. Among the most active compounds, 2i displayed similar ''in vitro'' growth inhibition in cancer cells independent of the cells' levels of resistance to proapoptotic stimuli and was found to be cytostatic in melanoma cell lines. Compound 2i was then tested by the National Cancer Institute Human Tumor Cell Line Anti-Cancer Drug Screen, and the NCI COMPARE algorithm did not reveal any correlation between its growth inhibition profiles with the NCI database compound profiles. The use of transcriptomically characterized melanoma models then enabled us to highlight mitochondrial targeting by 2i. This hypothesis was further confirmed by reactive oxygen production measurement and oxygen consumption analysis. | |abstract=We designed and synthesized 48 aryl-1H-imidazole derivatives and investigated their ''in vitro'' growth inhibitory activity in cancer cell lines known to present various levels of resistance to proapoptotic stimuli. The IC50 ''in vitro'' growth inhibitory concentration of these compounds ranged from >100 ΞΌM to single digit ΞΌM. Among the most active compounds, 2i displayed similar ''in vitro'' growth inhibition in cancer cells independent of the cells' levels of resistance to proapoptotic stimuli and was found to be cytostatic in melanoma cell lines. Compound 2i was then tested by the National Cancer Institute Human Tumor Cell Line Anti-Cancer Drug Screen, and the NCI COMPARE algorithm did not reveal any correlation between its growth inhibition profiles with the NCI database compound profiles. The use of transcriptomically characterized melanoma models then enabled us to highlight mitochondrial targeting by 2i. This hypothesis was further confirmed by reactive oxygen production measurement and oxygen consumption analysis. | ||
|keywords=SKMEl-28 cells | |||
|mipnetlab=BE Liege Votion DM | |mipnetlab=BE Liege Votion DM | ||
}} | }} | ||
{{Labeling | {{Labeling | ||
|area=Respiration | |||
|diseases=Cancer | |||
|organism=Human | |||
|tissues=Endothelial;epithelial;mesothelial cell, Other cell lines | |||
|preparations=Intact cells | |||
|couplingstates=ROUTINE | |||
|instruments=Oxygraph-2k | |instruments=Oxygraph-2k | ||
}} | }} | ||
Latest revision as of 14:20, 9 November 2016
| Mathieu V, Van Den Berge E, Ceusters Justine D, Konopka T, Cops A, Bruyère C, Pirker C, Berger W, Trieu-Van T, Serteyn D, Kiss R, Robiette R (2013) New 5-Aryl-1H-imidazoles display in vitro antitumor activity against apoptosis-resistant cancer models, including melanomas, through mitochondrial targeting. J Med Chem 56:6626-37. |
Mathieu V, Van Den Berge E, Ceusters Justine D, Konopka T, Cops A, Bruyere C, Pirker C, Berger W, Trieu-Van T, Serteyn D, Kiss R, Robiette R (2013) J Med Chem
Abstract: We designed and synthesized 48 aryl-1H-imidazole derivatives and investigated their in vitro growth inhibitory activity in cancer cell lines known to present various levels of resistance to proapoptotic stimuli. The IC50 in vitro growth inhibitory concentration of these compounds ranged from >100 ΞΌM to single digit ΞΌM. Among the most active compounds, 2i displayed similar in vitro growth inhibition in cancer cells independent of the cells' levels of resistance to proapoptotic stimuli and was found to be cytostatic in melanoma cell lines. Compound 2i was then tested by the National Cancer Institute Human Tumor Cell Line Anti-Cancer Drug Screen, and the NCI COMPARE algorithm did not reveal any correlation between its growth inhibition profiles with the NCI database compound profiles. The use of transcriptomically characterized melanoma models then enabled us to highlight mitochondrial targeting by 2i. This hypothesis was further confirmed by reactive oxygen production measurement and oxygen consumption analysis. β’ Keywords: SKMEl-28 cells
β’ O2k-Network Lab: BE Liege Votion DM
Labels: MiParea: Respiration
Pathology: Cancer
Organism: Human Tissue;cell: Endothelial;epithelial;mesothelial cell, Other cell lines Preparation: Intact cells
Coupling state: ROUTINE
HRR: Oxygraph-2k
