Discovery of (R)‑8-(1-(3,5-Difluorophenylamino)ethyl)‑N,N‑dimethyl-2-morpholino-4-oxo‑4H‑chromene-6-carboxamide (AZD8186): A Potent and Selective Inhibitor of PI3Kβ and PI3Kδ for the Treatment of PTEN-Deficient Cancers

Several studies have highlighted the dependency of PTEN deficient tumors to PI3Kβ activity and specific inhibition of PI3Kδ has been shown activity against human B-cell cancers. We describe the discovery and optimization of a series of 8-(1-anilino)ethyl)-2-morpholino-4-oxo-4H-chromene-6-carboxamide...

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Veröffentlicht in:	Journal of medicinal chemistry 2015-01, Vol.58 (2), p.943-962
Hauptverfasser:	Barlaam, Bernard, Cosulich, Sabina, Degorce, Sébastien, Fitzek, Martina, Green, Stephen, Hancox, Urs, Lambert-van der Brempt, Christine, Lohmann, Jean-Jacques, Maudet, Mickaël, Morgentin, Rémy, Pasquet, Marie-Jeanne, Péru, Aurélien, Plé, Patrick, Saleh, Twana, Vautier, Michel, Walker, Mike, Ward, Lara, Warin, Nicolas
Format:	Artikel
Sprache:	eng
Schlagworte:	Aniline Compounds - chemical synthesis Aniline Compounds - pharmacology Animals Chromones - chemical synthesis Chromones - pharmacology Class Ia Phosphatidylinositol 3-Kinase - antagonists & inhibitors Dogs Drug Discovery Humans Male Mice Neoplasms, Experimental - chemistry Neoplasms, Experimental - drug therapy PTEN Phosphohydrolase - deficiency Structure-Activity Relationship
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