Yun Ding; G. Joseph Franklin; Jennifer L. DeLorey; Paolo A. Centrella; Sibongile Mataruse; Matthew A. Clark; Steven R. Skinner; Svetlana L. Belyanskaya
ACS Comb. Sci., 2016, 18, 625−629
https://doi.org/10.1021/acscombsci.6b00078

Abstract

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).