一种铑（III）配合物作为神经前体细胞表达的、发育性下调的8-激活酶的抑制剂，对炎症性肠病具有体内活性。
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.
作者信息
Zhong Hai-Jing, Wang Wanhe, Kang Tian-Shu, Yan Hui, Yang Yali, Xu Lipeng, Wang Yuqiang, Ma Dik-Lung, Leung Chung-Hang
机构信息
State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau , Taipa, Macao P. R China.
Department of Chemistry, Hong Kong Baptist University , T1303, Cha Chi-Ming Science Tower, Kowloon Tong, Hong Kong, P. R. China.
出版信息
J Med Chem. 2017 Jan 12;60(1):497-503. doi: 10.1021/acs.jmedchem.6b00250. Epub 2016 Dec 23.
We report herein the identification of the rhodium(III) complex [Rh(phq)(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.
我们在此报告，铑（III）配合物[Rh(phq)(MOPIP)]（1）被鉴定为一种强效且选择性的ATP竞争性神经前体细胞表达、发育下调8（NEDD8）激活酶（NAE）抑制剂。构效关系分析表明，配合物1的整体有机金属设计对其抗炎活性很重要。配合物1在体内对炎症性肠病的潜在治疗显示出有前景的抗炎活性。
Zotero 插件