2. Academic Validation
  3. Design and Synthesis of Biaryl DNA-Encoded Libraries

Design and Synthesis of Biaryl DNA-Encoded Libraries

  • ACS Comb Sci. 2016 Oct 10;18(10):625-629. doi: 10.1021/acscombsci.6b00078.
Yun Ding 1,  G Joseph Franklin 1,  Jennifer L DeLorey 1,  Paolo A Centrella 1,  Sibongile Mataruse 1,  Matthew A Clark 1,  Steven R Skinner 1,  Svetlana Belyanskaya 1
Affiliations

Affiliation

  • 1 GlaxoSmithKline , Platform Technology & Science, ELT-Boston, 830 Winter Street, Waltham, Massachusetts 02451, United States.
PMID: 27571034 DOI: 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).

Keywords

DNA-encoded library technology; Suzuki−Miyaura cross-coupling.

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