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

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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

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

Bioorg Med Chem Lett. 2004 Feb 9;14(3):783-6.

PubMed ID

14741289 [ View in PubMed

]

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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Sorafenib	RAF proto-oncogene serine/threonine-protein kinase	IC 50 (nM)	12	N/A	N/A	Details