期刊
ORGANIC & BIOMOLECULAR CHEMISTRY
卷 14, 期 16, 页码 3889-3905出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c6ob00471g
关键词
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资金
- Marloes Technologies Ltd
- University of Nottingham
- Carroll University
- Cancer Research UK [C309/A11566]
- EPSRC [EP/K038869/1] Funding Source: UKRI
- Cancer Research UK [11566] Funding Source: researchfish
- Engineering and Physical Sciences Research Council [EP/K038869/1] Funding Source: researchfish
The imidazole ring is widespread in biologically active compounds, and hence imidazole-containing scaffolds are useful starting points for drug discovery programmes. We report the synthesis of a series of novel imidazole-containing compounds fused with either phenanthrene or phenanthroline, which show enhanced growth inhibitory potency against human colon, breast and melanoma cancer cell lines, as well as evidence of inhibition of the molecular chaperone heat shock protein 70 (Hsp70) pathway in cells, as shown by depletion of downstream oncogenic client proteins of the Hsp90 chaperone pathway, and induction of apoptosis.
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