Highly potent and selective 3-N-methylquinazoline-4(3H)-one based inhibitors of B-Raf(V600E) kinase

Herein we describe the design of a novel series of ATP competitive B-Raf inhibitors via structure-based methods. These 3-N-methylquinazoline-4(3H)-one based inhibitors exhibit both excellent cellular potency and striking B-Raf selectivity. Optimization led to the identification of compound 16, a pot...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2014-04, Vol.24 (8), p.1923-1927
Hauptverfasser:	Wenglowsky, Steve, Ren, Li, Grina, Jonas, Hansen, Joshua D, Laird, Ellen R, Moreno, David, Dinkel, Victoria, Gloor, Susan L, Hastings, Gregg, Rana, Sumeet, Rasor, Kevin, Sturgis, Hillary L, Voegtli, Walter C, Vigers, Guy, Willis, Brandon, Mathieu, Simon, Rudolph, Joachim
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Crystallography, X-Ray Drug Design Enzyme Activation - drug effects Humans Inhibitory Concentration 50 Molecular Structure Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Proto-Oncogene Proteins B-raf - antagonists & inhibitors Quinazolines - chemical synthesis Quinazolines - chemistry Quinazolines - pharmacology Tumor Burden - drug effects Xenograft Model Antitumor Assays
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Schreiben Sie den ersten Kommentar!