Terephthalamide derivatives as mimetics of the helical region of Bak peptide target Bcl-xL protein

A group of novel Bcl-xL/Bak antagonists, based on a terephthalamide scaffold, were designed to mimic the α-helical region of the Bak peptide. Good in vitro inhibition potencies in disrupting the Bak/Bcl-xL complex have been observed (terephthalamide 4, Ki=0.78±0.07 μM).