Yun Ding, G Joseph Franklin, Jennifer L DeLorey, Paolo A Centrella, Sibongile Mataruse, Matthew A Clark, Steven R Skinner, Svetlana Belyanskaya
DNA-encoded library technology (ELT) is a powerful tool for the discovery of new small-molecule ligands to various protein targets. Here we report the design and synthesis of biaryl DNA-encoded libraries based on the scaffold of 5-formyl 3-iodobenzoic acid. Three reactions on DNA template, acylation, Suzuki-Miyaura coupling and reductive amination, were applied in the library synthesis. The three cycle library of 3.5 million diversity has delivered potent hits for phosphoinositide 3-kinase α (PI3Kα).
October 10, 2016: ACS Combinatorial Science