Inhibitors of NF-kappaB derived from thalidomide.
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.
de-Blanco
Esperanza J Carcache
EJ
Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA.
Pandit
Bulbul
B
Hu
Zhigen
Z
Shi
Jiandong
J
Lewis
Andrew
A
Li
Pui-Kai
PK
D006367:HeLa Cells; D006801:Humans; D016328:NF-kappa B / Q000037:antagonists & inhibitors*; D013792:Thalidomide / Q000737:chemistry / Q000494:pharmacology*
D016328:NF-kappa B; D013792:Thalidomide