Isoflavone derivatives inhibit NF-κB-dependent transcriptional activity

✍ Scribed by Sunhee Lee; Kyung Chan Lim; Soon Young Shin; Young Han Lee

• Book ID: 104004811
• Publisher: Elsevier Science
• Year: 2010
• Tongue: English
• Weight: 463 KB
• Volume: 20
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/j.bmcl.2010.08.089

✦ Synopsis

The transcription factor NF-κB regulates diverse biological activities, such as inflammatory responses, cell proliferation, and cell survival. Isoflavones are known to have anti-inflammatory and anti-tumor activities, due, in part, to inhibition of NF-κB activity. However, the structural moiety of isoflavones responsible for the inhibition of NF-κB is not clearly understood. In this work, structure-activity relationships of isoflavone derivatives were examined with regard to NF-κB inhibition, using CoMFA and CoMSIA. The results show that substituents at the C-7 and C-4' positions are crucial for the inhibition of TNFα-induced transcriptional activity of NF-κB.