Diversity-Oriented Synthesis as a Strategy for Fragment Evolution against GSK3β.
ACS Med Chem Lett
| Authors | |
| 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. |
| Year of Publication | 2016
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| Journal | ACS Med Chem Lett
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| Volume | 7
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| Issue | 9
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| Pages | 852-6
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| Date Published | 2016 Sep 08
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| DOI | 10.1021/acsmedchemlett.6b00230
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| PubMed ID | 27660690
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| PubMed Central ID | PMC5018862
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| Links | |
| Grant list | P30 DK020541 / DK / NIDDK NIH HHS / United States
T32 GM007288 / GM / NIGMS NIH HHS / United States
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