Journal
CURRENT PHARMACEUTICAL DESIGN
Volume 8, Issue 25, Pages 2269-2278Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1381612023393125
Keywords
diphenyl ureas; BAY 43-9006; Raf-1 kinase; cancer; Ras
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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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