Design and synthesis of 5,6-fused heterocyclic amides as Raf kinase inhibitors

Two scaffolds based on 5,6-fused heterocyclic backbones were designed and synthesized as Raf kinase inhibitors. The scaffolds were assessed for in vitro pan–Raf inhibition, activity in cell proliferation and target modulation assays, and pharmacokinetic parameters. Two scaffolds based on 5,6-fused h...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-06, Vol.21 (11), p.3286-3289
Hauptverfasser:	Ramurthy, Savithri, Aikawa, Mina, Amiri, Payman, Costales, Abran, Hashash, Ahmad, Jansen, Johanna M., Lin, Song, Ma, Sylvia, Renhowe, Paul A., Shafer, Cynthia M., Subramanian, Sharadha, Sung, Leonard, Verhagen, Joelle
Format:	Artikel
Sprache:	eng
Schlagworte:	5,6-Fused heterocycles amides Amides - chemical synthesis Amides - chemistry Amides - pharmacology Antineoplastic agents Benzothiazoles Benzoxazoles Binding Sites Biological and medical sciences Cell Proliferation Drug Design Enzyme Activation - drug effects Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology General aspects Heterocyclic Compounds - chemical synthesis Heterocyclic Compounds - chemistry Heterocyclic Compounds - pharmacology Medical sciences Models, Molecular Molecular Structure Pharmacokinetic profile pharmacokinetics Pharmacology. Drug treatments Raf kinase inhibitors raf Kinases - antagonists & inhibitors Structure-Activity Relationship
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Zusammenfassung:	Two scaffolds based on 5,6-fused heterocyclic backbones were designed and synthesized as Raf kinase inhibitors. The scaffolds were assessed for in vitro pan–Raf inhibition, activity in cell proliferation and target modulation assays, and pharmacokinetic parameters. Two scaffolds based on 5,6-fused heterocyclic backbones were designed and synthesized as Raf kinase inhibitors. The scaffolds were assessed for in vitro pan–Raf inhibition, activity in cell proliferation and target modulation assays, and pharmacokinetic parameters.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2011.04.023