Diversity-Oriented Synthesis as a Strategy for Fragment Evolution against GSK3β
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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