新型乙内酰脲作为肿瘤坏死因子-α转化酶（TACE）选择性非异羟肟酸抑制剂的发现。
Discovery of novel hydantoins as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
作者信息
Sheppeck James E, Gilmore John L, Yang Anle, Chen Xiao-Tao, Xue Chu-Biao, Roderick John, Liu Rui-Qin, Covington Maryanne B, Decicco Carl P, Duan James J-W
机构信息
Bristol-Myers Squibb Pharmaceutical Research Institute, Discovery Chemistry, PO Box 4000, Princeton, NJ 08543-4000, USA.
出版信息
Bioorg Med Chem Lett. 2007 Mar 1;17(5):1413-7. doi: 10.1016/j.bmcl.2006.11.089. Epub 2006 Dec 2.
A series of novel hydantoins was designed and synthesized as structural alternatives to hydroxamate inhibitors of TACE. 5-Mono- and di-substituted hydantoins exhibited activity with IC50 values of 11-60 nM against porcine TACE in vitro and excellent selectivity against other MMPs.
设计并合成了一系列新型乙内酰脲，作为TACE异羟肟酸酯抑制剂的结构替代物。5-单取代和二取代乙内酰脲在体外对猪TACE表现出活性，IC50值为11 - 60 nM，并且对其他基质金属蛋白酶具有优异的选择性。
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