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

Author(s)
Zhong, Cheng; Ramek, Alexander; Koehler, Angela Nicole
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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.
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Abstract
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
2016-07
URI
https://hdl.handle.net/1721.1/126533
Department
Massachusetts Institute of Technology. Department of Biological Engineering
Journal
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

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