期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 59, 期 8, 页码 4026-4031出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.6b00112
关键词
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资金
- Hong Kong Baptist University [FRG2/14-15/004, FRG2/15-16/002]
- Health and Medical Research Fund [HMRF/14130522]
- Research Grants Council [HKBU/201811, HKBU/204612, HKBU/201913]
- French Agence Nationale de la Recherche/Research Grants Council Joint Research Scheme [AHKBU201/12, Oligoswitch ANR-12-IS07-0001]
- National Natural Science Foundation of China [21575121]
- Guangdong Province Natural Science Foundation [2015A030313816]
- Hong Kong Baptist University Century Club
- Interdisciplinary Research Matching Scheme [RC-IRMS/14-15/06]
- Science and Technology Development Fund, Macao SAR [103/2012/A3]
- University of Macau [MYRG091(Y3-L2)-ICMS12-LCH, MYRG2015-00137-ICMS-QRCM, MRG023/LCH/2013/ICMS, MRG044/LCH/2015/ICMS]
The novel iridium(III) complex 1 was verified as a potent inhibitor of the TNF-alpha TNFR protein protein interaction in vitro and in cellulo. The iridium(III) center plays a critical role in organizing the structure of the bioactive metal complex, as the isolated ligands were found to be completely inactive. Both iridium enantiomers inhibited TNF-ainduced NF-kappa B activity and TNF-alpha TNFR binding. 1 represents a promising scaffold for the further development of more potent organometallic TNF-alpha inhibitors.
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