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

S Ramurthy, A Costales, JM Jansen, B Levine…

Index: Ramurthy, Savithri; Costales, Abran; Jansen, Johanna M.; Levine, Barry; Renhowe, Paul A.; Shafer, Cynthia M.; Subramanian, Sharadha Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 4 p. 1678 - 1681

Full Text: HTML

Citation Number: 12

Abstract

Compounds belonging to several scaffolds—quinazolines, quinolines and quinoxalines— were designed and synthesized as Raf kinase inhibitors. Scaffolds were assessed for in vitro BrafV600E inhibition, and overall kinase selectivity. Pharmacokinetic parameters for one of the scaffolds were also determined.

Related Articles:

A novel and practical synthesis of 2-amino-5-hydroxypropiophenone

[Xiong, Xiao-Dong; Chen, Wen-Xue; Kuang, Yun-Yan; Chen, Fen-Er Organic Preparations and Procedures International, 2009 , vol. 41, # 5 p. 423 - 427]

Toward new camptothecins. Part 6: Synthesis of crucial ketones and their use in Friedländer reaction

[Gavara, Laurent; Boisse, Thomas; Henichart, Jean-Pierre; Daich, Adam; Rigo, Benoit; Gautret, Philippe Tetrahedron, 2010 , vol. 66, # 38 p. 7544 - 7561]

2-amino and 2'-aminocombretastatin derivatives as potent antimitotic agents

[Journal of Medicinal Chemistry, , vol. 49, # 21 p. 6412 - 6415]

Synthesis and structure–activity relationships of thioflavone derivatives as specific inhibitors of the ERK-MAP kinase signaling pathway

[Bioorganic and Medicinal Chemistry, , vol. 12, # 9 p. 2397 - 2407]

Preparation of nitrobenzaldehydes and nitrophenyl ketones by electrophilic amination of nitrobenzyl aryl sulfones

[Liebigs Annalen der Chemie, , # 6 p. 537 - 538]

More Articles...