发现β-苯甲酰胺基异羟肟酸作为强效、选择性且口服生物可利用的肿瘤坏死因子-α转换酶抑制剂。
Discovery of beta-benzamido hydroxamic acids as potent, selective, and orally bioavailable TACE inhibitors.
作者信息
Duan James J-W, Chen Lihua, Lu Zhonghui, Xue Chu-Biao, Liu Rui-Qin, Covington Maryanne B, Qian Mingxin, Wasserman Zelda R, Vaddi Krishna, Christ David D, Trzaskos James M, Newton Robert C, Decicco Carl P
机构信息
Research and Development, Bristol-Myers Squibb Company, Princeton, NJ 08543-4000, USA.
出版信息
Bioorg Med Chem Lett. 2008 Jan 1;18(1):241-6. doi: 10.1016/j.bmcl.2007.10.093. Epub 2007 Oct 30.
Beta-benzamido hydroxamic acids were discovered as potent TACE inhibitors. A computer model was constructed to help understanding the binding activities and guiding SAR study. SAR optimization led to the discovery of compound 30 which met all in vitro and in vivo criteria for the program and was selected for further evaluation.
β-苯甲酰胺基异羟肟酸被发现是有效的肿瘤坏死因子-α转换酶（TACE）抑制剂。构建了一个计算机模型以帮助理解其结合活性并指导构效关系（SAR）研究。通过构效关系优化发现了化合物30，它满足该项目的所有体外和体内标准，并被选作进一步评估。
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