Discovery of Bivalent Kinase Inhibitors via Enzyme-Templated Fragment Elaboration

[Image: see text] We have employed novel fragment-based screening methodology to discover bivalent kinase inhibitors with improved selectivity. Starting from a low molecular weight promiscuous kinase inhibitor, we appended a thiol for subsequent reaction with a library of acrylamide electrophiles. E...

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Bibliographic Details
Published in:ACS Med Chem Lett
Main Authors: Kwarcinski, Frank E., Steffey, Michael E., Fox, Christel C., Soellner, Matthew B.
Format: Artigo
Language:Inglês
Published: American Chemical Society 2015
Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC4538437/
https://ncbi.nlm.nih.gov/pubmed/26286460
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.5b00167
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