期刊
CHEMICAL COMMUNICATIONS
卷 51, 期 84, 页码 15458-15461出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c5cc06095h
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资金
- Cancer Research UK
- Royal Society Dorothy Hodgkin fellowship
- SGC
- NIH
- Friends of the Cancer Center
- Welch Foundation
- CPRIT
- BBSRC [BB/L004275/1] Funding Source: UKRI
- EPSRC [EP/L003376/1] Funding Source: UKRI
- Biotechnology and Biological Sciences Research Council [BB/L004275/1] Funding Source: researchfish
- British Heart Foundation [PG/12/33/29546, RG/11/1/28684] Funding Source: researchfish
- Cancer Research UK [16466, 18245] Funding Source: researchfish
- Engineering and Physical Sciences Research Council [EP/L003376/1] Funding Source: researchfish
There is interest in developing potent, selective, and cell-permeable inhibitors of human ferrous iron and 2-oxoglutarate (2OG) oxygenases for use in functional and target validation studies. The 3-component Betti reaction enables efficient one-step C-7 functionalisation of modified 8-hydroxyquinolines (8HQs) to produce cell-active inhibitors of KDM4 histone demethylases and other 2OG oxygenases; the work exemplifies how a template-based metallo-enzyme inhibitor approach can be used to give biologically active compounds.
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