期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 7, 期 9, 页码 852-856出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.6b00230
关键词
Diversity oriented synthesis; fragment-based drug discovery; fragment growing GSK3 beta
资金
- Broad Institute SPARC Grant
- NIH/NIMH [R01MH091115]
- Tau Consortium
- Barrus Foundation
- NIH/NIGMS [U54 GM094662]
- NIH/NCI [P30 CA013330]
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 GSK3 beta 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.
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