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

Yikai Wang, Jean Yves Wach, Patrick Sheehan, Cheng Zhong, Chenyang Zhan, Richard Harris, Steven C. Almo, Joshua Bishop, Stephen J. Haggarty, Alexander Ramek, Kayla N. Berry, Conor O'Herin, Angela N. Koehler, Alvin W. Hung, Damian W. Young

Research output: Contribution to journalArticlepeer-review

32 Scopus citations


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.

Original languageEnglish (US)
Pages (from-to)852-856
Number of pages5
JournalACS Medicinal Chemistry Letters
Issue number9
StatePublished - Sep 8 2016


  • Diversity oriented synthesis
  • GSK3β
  • fragment growing
  • fragment-based drug discovery

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry


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