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Design and Discovery of Small Molecules Targeting Raf-1 Kinase

Author(s): Timothy B. Lowinger, Bernd Riedl, Jacques Dumas and Roger A. Smith

Affiliation: Bayer AG, Pharma Research Center, D-42096, Wuppertal, Germany

Keywords: diphenyl ureas, bay 43-9006, raf-1 kinase, cancer, ras

Abstract:

Raf kinase, an enzyme which acts downstream in the Ras signaling pathway, is involved in cancerous cell proliferation. Thus, small molecule inhibitors of Raf kinase activity may be important agents for the treatment of cancer. A novel class of Raf-1 inhibitors was discovered, using a combination of medicinal and combinatorial chemistry approaches. This effort culminated in the identification of the clinical candidate BAY 43-9006, currently undergoing Phase I clinical trials. The present review summarizes the medicinal chemistry development of ureas as highly potent inhibitors of Raf-1 kinase.

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Article Details

VOLUME: 8
ISSUE: 25
Page: [2269 - 2278]
Pages: 10
DOI: 10.2174/1381612023393125