Development Of Potent B-Raf(V600e) Inhibitors Containing An Arylsulfonamide Headgroup

John C. Stellwagen,George M. Adjabeng,Marc R. Arnone,Scott H. Dickerson,Chao Han,Keith R. Hornberger,Alastair J. King,Robert A. Mook,Kimberly G. Petrov,Tara R. Rheault,Cynthia M. Rominger,Olivia W. Rossanese,Kimberly N. Smitheman,Alex G. Waterson,David E. Uehling

Bioorganic & medicinal chemistry letters（2011）

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摘要

A potent series of inhibitors against the B-RafV600E kinase have been developed that show excellent activity in cellular assays and good oral bioavailability in rats. The key structural features of the series are an arylsulfonamide headgroup, a thiazole core, and a fluorine ortho to the sulfonamide nitrogen. Crown Copyright (C) 2011 Published by Elsevier Ltd. All rights reserved.

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B-RafV600E,Sulfonamide,Thiazole

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