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

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• 作者：Hai-Jing Zhong ; Wanhe Wang ; Tian-Shu Kang ; Hui Yan ; Yali Yang ; Lipeng Xu ; Yuqiang Wang ; Dik-Lung MaChung-Hang Leung
• 刊名：Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：January 12, 2017
• 年：2017
• 卷：60
• 期：1
• 页码：497-503
• 全文大小：395K
• ISSN：1520-4804

文摘

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.