4.7 Article

A Rhodium(III) Complex as an Inhibitor of Neural Precursor Cell Expressed, Developmentally Down-Regulated 8-Activating Enzyme with in Vivo Activity against Inflammatory Bowel Disease

期刊

JOURNAL OF MEDICINAL CHEMISTRY
卷 60, 期 1, 页码 497-503

出版社

AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.6b00250

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资金

  1. Hong Kong Baptist University [FRG2/15-16/002]
  2. Health and Medical Research Fund [HMRF/14130522]
  3. Research Grants Council [HKBU/12301115, HKBU/204612, HKBU/201913]
  4. French National Research Agency/Research Grants Council Joint Research Scheme [A-HKBU201/12 - Oligoswitch]
  5. National Natural Science Foundation of China [21575121]
  6. Guangdong Province Natural Science Foundation [2015A030313816]
  7. Hong Kong Baptist University Century Club [RC-IRMS/15-16/03]
  8. Science and Technology Development Fund, Macao SAR [098/2014/A2]
  9. University of Macau [MYRG2015-00137-ICMS-ARCM, MYRG2016-00151-ICMS-QRCM, MRG044/LCH/2015/ICMS]

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We report herein the identification of the rhodium(III) complex [Rh(phq)(2)(MOPIP)](+) (1): as a potent and selective ATP-competitive neural precursor cell expressed developmentally down-regulated 8 (NEDD8)-activating enzyme (NAE) inhibitor. Structure-activity relationship analysis indicated that the overall organometallic design of complex 1 was important for anti-inflammatory, activity. Complex 1 showed promising anti-inflammatory activity in vivo for the potential treatment of inflammatory bowel disease.

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