Design and Synthesis of Biaryl DNA-Encoded Libraries

被引：51
|
作者：
Ding, Yun [1 ]
Franklin, G. Joseph [1 ]
DeLorey, Jennifer L. [1 ,2 ]
Centrella, Paolo A. [1 ,3 ]
Mataruse, Sibongile [1 ,4 ]
Clark, Matthew A. [1 ,3 ]
Skinner, Steven R. [1 ]
Belyanskaya, Svetlana [1 ]
机构：
[1] GlaxoSmithKline, Platform Technol & Sci, ELT Boston, 830 Winter St, Waltham, MA 02451 USA
[2] Tedor Pharma Inc, 400 Highland Corp Dr, Cumberland, RI 02864 USA
[3] X Chem Inc, 100 Beaver St, Waltham, MA 02453 USA
[4] 419 Main St, Wareham, MA 02571 USA
来源：
ACS COMBINATORIAL SCIENCE | 2016年 / 18卷 / 10期
关键词：
Suzuki-Miyaura cross-coupling; DNA-encoded library technology; CHEMICAL LIBRARIES; TECHNOLOGY ELT; DISCOVERY; INHIBITORS; SELECTION; IDENTIFICATION; ANTAGONISTS; CHEMISTRY; POTENT;
D O I：
10.1021/acscombsci.6b00078
中图分类号：
O69 [应用化学];
学科分类号：
081704 ;
摘要：
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-forrnyl 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 alpha (PI3K alpha).
引用
收藏
页码：625 / 629
页数：5
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