α,α-二氟-β-酮膦酸酯作为蛋白酪氨酸磷酸酶1B的有效抑制剂。
Alpha,alpha-difluoro-beta-ketophosphonates as potent inhibitors of protein tyrosine phosphatase 1B.
作者信息
Li Xianfeng, Bhandari Ashok, Holmes Christopher P, Szardenings Anna K
机构信息
Affymax, Inc., 4001 Miranda Avenue, Palo Alto, CA 94304, USA.
出版信息
Bioorg Med Chem Lett. 2004 Aug 16;14(16):4301-6. doi: 10.1016/j.bmcl.2004.05.082.
A novel series of inhibitors that contain an aryl alpha,alpha-difluoro-beta-ketophosphonate group has been synthesized and evaluated against protein tyrosine phosphatase 1B. These compounds exhibit strong inhibitory activity, the best of which has a K(i) value of 0.17 microM. These results demonstrate that aryl alpha,alpha-difluoro-beta-ketophosphonates are powerful phosphotyrosine mimetics for the development of potent PTP inhibitors.
已合成了一系列含有芳基α,α-二氟-β-酮膦酸酯基团的新型抑制剂，并对其针对蛋白酪氨酸磷酸酶1B进行了评估。这些化合物表现出很强的抑制活性，其中最佳者的K(i)值为0.17微摩尔。这些结果表明，芳基α,α-二氟-β-酮膦酸酯是用于开发强效蛋白酪氨酸磷酸酶抑制剂的强大磷酸酪氨酸模拟物。
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