Discovery of bioactive molecules from CuAAC click-chemistry-based combinatorial libraries

作者：Wang, Xueshun; Huang, Boshi; Liu, Xinyong^*; Zhan, Peng^*

来源：Drug Discovery Today, 2016, 21(1): 118-132.

DOI：10.1016/j.drudis.2015.08.004

• AZIDE-ALKYNE CYCLOADDITION
• MATRIX METALLOPROTEASE INHIBITORS
• PROTEIN-TYROSINE PHOSPHATASES
• IN-SITU
• DRUG DISCOVERY
• CHEMICAL-BIOLOGY
• RAPID DISCOVERY
• 1,5-DISUBSTITUTED 1,2,3-TRIAZOLES
• INDOLEAMINE 2,3-DIOXYGENASE
• PRIVILEGED STRUCTURES

The rapid assembly and in situ screening of focused combinatorial fragment libraries using CuAAC click chemistry is a highly robust and efficient strategy for establishing SAR and for discovering bioactive molecules. This review outlines the current status of this methodology in drug discovery application. The inherent limitations, challenges and prospects are critically discussed.

• 出版日期2016-1
• 单位山东大学