Inhibitors of NF-kappaB derived from thalidomide

  • Bioorg Med Chem Lett. 2007 Nov 1;17(21):6031-5. doi: 10.1016/j.bmcl.2007.01.088.
Esperanza J Carcache de-Blanco  1 ,  Bulbul Pandit ,  Zhigen Hu ,  Jiandong Shi ,  Andrew Lewis ,  Pui-Kai Li
Affiliations
  • 1. Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA.
PMID: 17845850 DOI: 10.1016/j.bmcl.2007.01.088
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.