Design and modular parallel synthesis of a MCR derived α-helix mimetic protein–protein interaction inhibitor scaffold

A terphenyl α-helix mimetic scaffold recognized to be capable of disrupting protein–protein interactions was structurally morphed into an easily amenable and versatile multicomponent reaction (MCR) backbone. The design, modular in-parallel library synthesis, initial cell based biological data, and preliminary in vitro screening for the disruption of the Bcl-w/Bak protein–protein interaction by representatives of the MCR derived scaffold are presented.

Design, synthesis and biological activity of Bcl family imidazole protein interaction antagonists is reported.Figure optionsDownload as PowerPoint slide