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源自沙利度胺的核因子κB抑制剂。

Inhibitors of NF-kappaB derived from thalidomide.

作者信息

de-Blanco Esperanza J Carcache, Pandit Bulbul, Hu Zhigen, Shi Jiandong, Lewis Andrew, Li Pui-Kai

机构信息

Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA.

出版信息

Bioorg Med Chem Lett. 2007 Nov 1;17(21):6031-5. doi: 10.1016/j.bmcl.2007.01.088. Epub 2007 Feb 2.

Abstract

A series of compounds originally derived from thalidomide were synthesized and evaluated. The most potent compounds in this series, 5HPP-33 and compound 20, inhibited NF-kappaB activation in HeLa cells. Preliminary study indicated that the mechanism of inhibition of NF-kappaB activation is through inhibition of its translocation from the cytoplasm to the nucleus.

摘要

合成并评估了一系列最初衍生自沙利度胺的化合物。该系列中最有效的化合物5HPP - 33和化合物20,可抑制HeLa细胞中的NF-κB激活。初步研究表明,抑制NF-κB激活的机制是通过抑制其从细胞质向细胞核的转运。

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