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 |
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| container_title | ACS combinatorial science |
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| creator | Ding, Yun Franklin, G. Joseph DeLorey, Jennifer L Centrella, Paolo A Mataruse, Sibongile Clark, Matthew A Skinner, Steven R Belyanskaya, Svetlana |
| description | 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). |
| doi_str_mv | 10.1021/acscombsci.6b00078 |
| format | Article |
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| ispartof | ACS combinatorial science, 2016-10, Vol.18 (10), p.625-629 |
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| language | eng |
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| source | ACS Publications; MEDLINE |
| subjects | Acylation Amination Combinatorial Chemistry Techniques DNA - chemistry Humans Iodobenzoates - chemistry Ligands Phosphatidylinositol 3-Kinases - chemistry Small Molecule Libraries - chemical synthesis Structure-Activity Relationship |
| title | Design and Synthesis of Biaryl DNA-Encoded Libraries |
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