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ID: ALA1147437

Journal: Bioorg Med Chem Lett

Title: Omega-carboxypyridyl substituted ureas as Raf kinase inhibitors: SAR of the amide substituent.

Authors: Khire UR, Bankston D, Barbosa J, Brittelli DR, Caringal Y, Carlson R, Dumas J, Gane T, Heald SL, Hibner B, Johnson JS, Katz ME, Kennure N, Kingery-Wood J, Lee W, Liu XG, Lowinger TB, McAlexander I, Monahan MK, Natero R, Renick J, Riedl B, Rong H, Sibley RN, Smith RA, Wolanin D.

Abstract: Bis-aryl ureas have been disclosed previously as a potent class of Raf kinase inhibitors. Modifications in the amide portion led to an improvement in aqueous solubility, an important characteristic for an oral drug. Based on this finding, we hypothesize that this portion of the molecule is directed towards the solvent in Raf-1.

CiteXplore: 14741289

DOI: 10.1016/j.bmcl.2003.11.041