Diversity-Oriented Synthesis as a Strategy for Fragment Evolution against GSK3β
Author(s)
Zhong, Cheng; Ramek, Alexander; Koehler, Angela Nicole
DownloadAccepted version (1.469Mb)
Publisher Policy
Publisher Policy
Article is made available in accordance with the publisher's policy and may be subject to US copyright law. Please refer to the publisher's site for terms of use.
Terms of use
Metadata
Show full item recordAbstract
Traditional fragment-based drug discovery (FBDD) relies heavily on structural analysis of the hits bound to their targets. Herein, we present a complementary approach based on diversity-oriented synthesis (DOS). A DOS-based fragment collection was able to produce initial hit compounds against the target GSK3β, allow the systematic synthesis of related fragment analogues to explore fragment-level structure-activity relationship, and finally lead to the synthesis of a more potent compound.
Date issued
2016-07Department
Massachusetts Institute of Technology. Department of Biological EngineeringJournal
ACS medicinal chemistry letters
Publisher
American Chemical Society (ACS)
Citation
Wang, Yikai et al. “Diversity-Oriented Synthesis as a Strategy for Fragment Evolution against GSK3β.” ACS medicinal chemistry letters, vol. 7, 2016, pp. 852-856 © 2016 The Author(s)
Version: Author's final manuscript
ISSN
1948-5875