Design and synthesis of 6,6-fused heterocyclic amides as raf kinase inhibitors.

Savithri Ramurthy, Abran Costales, Johanna M Jansen, Barry Levine, Paul A Renhowe, Cynthia M Shafer, Sharadha Subramanian

Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research, Emeryville, CA 94608, USA. savithri.ramurthy@novartis.com

Bioorganic & medicinal chemistry letters 2012 Feb 15

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Compounds belonging to several scaffolds-quinazolines, quinolines and quinoxalines-were designed and synthesized as Raf kinase inhibitors. Scaffolds were assessed for in vitro Braf(V600E) inhibition, and overall kinase selectivity. Pharmacokinetic parameters for one of the scaffolds were also determined. Copyright © 2011 Elsevier Ltd. All rights reserved.

Citation

Savithri Ramurthy, Abran Costales, Johanna M Jansen, Barry Levine, Paul A Renhowe, Cynthia M Shafer, Sharadha Subramanian. Design and synthesis of 6,6-fused heterocyclic amides as raf kinase inhibitors. Bioorganic & medicinal chemistry letters. 2012 Feb 15;22(4):1678-81