Design and Development of a Macrocyclic Series Targeting Phosphoinositide 3-Kinase δ

[Image: see text] A macrocyclization approach has been explored on a series of benzoxazine phosphoinositide 3-kinase δ inhibitors, resulting in compounds with improved potency, permeability, and in vivo clearance while maintaining good solubility. The thermodynamics of binding was explored via surfa...

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Veröffentlicht in:ACS Med Chem Lett
Hauptverfasser: Spencer, Jonathan A., Baldwin, Ian R., Barton, Nick, Chung, Chun-Wa, Convery, Máire A., Edwards, Christopher D., Jamieson, Craig, Mallett, David N., Rowedder, James E., Rowland, Paul, Thomas, Daniel A., Hardy, Charlotte J.
Format: Artigo
Sprache:Inglês
Veröffentlicht: American Chemical Society 2020
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC7357223/
https://ncbi.nlm.nih.gov/pubmed/32676144
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.0c00061
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