Structural Features Defining NF-κB Inhibition by Lignan-Inspired Benzofurans and Benzothiophenes

Abstract

A series of 2-arylbenzofurans and 2-arylbenzothiophenes was synthesized carrying three different side chains in position five. The synthesized compounds were tested for NF-κB inhibition to establish a structure activity relationship. It was found that both, the side chain in position five and the substitution pattern of the aryl moiety in position two have a significant influence on the inhibitory activity.

Keywords

• NF-κB inhibition
• natural product
• lignans
• cross-coupling
• C-H activation
• direct arylation