Diversity-Oriented Synthesis as a Strategy for Fragment Evolution against GSK3β
Name
ml6b00230.pdf
Description
Accepted version
Size
1.47 MB
Format
Adobe PDF
Checksum (MD5)
2a7e876d0b876bc7878dfe366d33ce5e
Author(s)
Zhong, Cheng
Ramek, Alexander
Koehler, Angela Nicole
Date Issued
July 2016
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
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.
MIT Department
Massachusetts Institute of Technology. Department of Biological Engineering
Terms of Use
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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DOI of Published Version
https://doi.org/10.1021/ACSMEDCHEMLETT.6B00230
