Literature DB >> 27660690

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

Yikai Wang1, Jean-Yves Wach1, Patrick Sheehan1, Cheng Zhong1, Chenyang Zhan2, Richard Harris2, Steven C Almo2, Joshua Bishop3, Stephen J Haggarty3, Alexander Ramek1, Kayla N Berry1, Conor O'Herin1, Angela N Koehler1, Alvin W Hung1, Damian W Young1.   

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.

Entities:  

Keywords:  Diversity oriented synthesis; GSK3β; fragment growing; fragment-based drug discovery

Year:  2016        PMID： 27660690      PMCID： PMC5018862          DOI： 10.1021/acsmedchemlett.6b00230

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  32 in total

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