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

Xueshun Wang; Boshi Huang; Xinyong Liu; Peng Zhan

doi:10.1016/j.drudis.2015.08.004

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

Drug Discov Today. 2016 Jan;21(1):118-132. doi: 10.1016/j.drudis.2015.08.004. Epub 2015 Aug 24.

Authors

Xueshun Wang¹, Boshi Huang¹, Xinyong Liu², Peng Zhan³

Affiliations

¹ Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012 Jinan, Shandong, China.
² Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012 Jinan, Shandong, China. Electronic address: [email protected].
³ Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012 Jinan, Shandong, China. Electronic address: [email protected].

PMID: 26315392
DOI: 10.1016/j.drudis.2015.08.004

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't
Review

MeSH terms

Click Chemistry / methods*
Combinatorial Chemistry Techniques / methods*
Drug Discovery*