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

A macrocyclization approach has been explored on a series of benzoxazine phosphoinositide 3-kinase delta inhibitors, resulting in compounds with improved potency, permeability, and in vivo clearance while maintaining good solubility. The thermodynamics of binding was explored via surface plasmon res...

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Veröffentlicht in:	ACS medicinal chemistry letters Jg. 11; H. 7; S. 1386 - 1391
Hauptverfasser:	Spencer, Jonathan A., Baldwin, Ian R., Barton, Nick, Chung, Chun-Wa, Convery, Maire A., Edwards, Christopher D., Jamieson, Craig, Mallett, David N., Rowedder, James E., Rowland, Paul, Thomas, Daniel A., Hardy, Charlotte J.
Format:	Journal Article
Sprache:	Englisch
Veröffentlicht:	WASHINGTON Amer Chemical Soc 09.07.2020
Schlagworte:	Chemistry, Medicinal Life Sciences & Biomedicine Pharmacology & Pharmacy Science & Technology Thermodynamics POTENT Lipid kinase OPTIMIZATION PI3K delta INHIBITORS BINDING DISCOVERY Macrocycle
ISSN:	1948-5875, 1948-5875
Online-Zugang:	Weitere Angaben
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