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. 2001 Oct 22;11(20):2775-8.
doi: 10.1016/s0960-894x(01)00571-6.

Discovery of heterocyclic ureas as a new class of raf kinase inhibitors: identification of a second generation lead by a combinatorial chemistry approach

R A Smith  1 , J Barbosa, C L Blum, M A Bobko, Y V Caringal, R Dally, J S Johnson, M E Katz, N Kennure, J Kingery-Wood, W Lee, T B Lowinger, J Lyons, V Marsh, D H Rogers, S Swartz, T Walling, H Wild
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Discovery of heterocyclic ureas as a new class of raf kinase inhibitors: identification of a second generation lead by a combinatorial chemistry approach

R A Smith et al. Bioorg Med Chem Lett. .

Abstract

Heterocyclic ureas, such as N-3-thienyl N'-aryl ureas, have been identified as novel inhibitors of raf kinase, a key mediator in the ras signal transduction pathway. Structure-activity relationships were established, and the potency of the screening hit was improved 10-fold to IC(50)=1.7 microM. A combinatorial synthesis approach enabled the identification of a breakthrough lead (IC(50)=0.54 microM) for a second generation series of heterocyclic urea raf kinase inhibitors.

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