Design and Synthesis of Biaryl DNA-Encoded Libraries

Design and Synthesis of Biaryl DNA-Encoded Libraries

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...

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Veröffentlicht in:ACS combinatorial science 2016-10, Vol.18 (10), p.625-629
Hauptverfasser: Ding, Yun, Franklin, G. Joseph, DeLorey, Jennifer L, Centrella, Paolo A, Mataruse, Sibongile, Clark, Matthew A, Skinner, Steven R, Belyanskaya, Svetlana
Format: Artikel
Sprache:eng
Schlagworte:
Acylation
Amination
Combinatorial Chemistry Techniques
DNA - chemistry
Humans
Iodobenzoates - chemistry
Ligands
Phosphatidylinositol 3-Kinases - chemistry
Small Molecule Libraries - chemical synthesis
Structure-Activity Relationship
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Zusammenfassung: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).
ISSN:2156-8952
2156-8944
DOI:10.1021/acscombsci.6b00078