肿瘤坏死因子-α转化酶（TACE）的选择性膦酰胺类抑制剂的发现。
Discovery of selective phosphonamide-based inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
作者信息
Sawa Masaaki, Kurokawa Kiriko, Inoue Yoshimasa, Kondo Hirosato, Yoshino Kohichiro
机构信息
Department of Chemistry, R&D Laboratories, Nippon Organon K.K., 1-5-90, Tomobuchi-cho, Miyakojima-ku, 16, Osaka 534-00, Japan.
出版信息
Bioorg Med Chem Lett. 2003 Jun 16;13(12):2021-4. doi: 10.1016/s0960-894x(03)00292-0.
A novel series of phosphonamide-based inhibitors of tumor necrosis factor-alpha converting enzyme (TACE) was discovered by structural modification of tetrahydroisoquinoline derivative 1b, which was extremely weak inhibitor of TACE. (S)-Isomer at the phosphorus atom (7b) displayed potent inhibition for TACE, while selectivity sparing MMP-1, -3, and -9.
通过对四氢异喹啉衍生物1b进行结构修饰，发现了一系列新型的基于磷酰胺的肿瘤坏死因子-α转化酶（TACE）抑制剂，1b是一种活性极低的TACE抑制剂。磷原子上的（S）-异构体（7b）对TACE表现出强效抑制作用，同时对基质金属蛋白酶-1、-3和-9具有选择性保留。
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