Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors.

doi:10.1021/jm101479y

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Article

Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors.

Journal of medicinal chemistry - 24 Mar 2011

Gould Alexandra E, Adams Ruth, Adhikari Sharmila, Aertgeerts Kathleen, Afroze Roushan, Blackburn Christopher, Calderwood Emily F, Chau Ryan, Chouitar Jouhara, Duffey Matthew O, England Dylan B, Farrer Cheryl, Forsyth Nancy, Garcia Khristofer, Gaulin Jeffery, Greenspan Paul D, Guo Ribo, Harrison Sean J, Huang Shih-Chung, Iartchouk Natalia, Janowick Dave, Kim Mi-Sook, Kulkarni Bheemashankar, Langston Steven P, Liu Jane X, Ma Li-Ting, Menon Saurabh, Mizutani Hirotake, Paske Erin, Renou Christelle C, Rezaei Mansoureh, Rowland R Scott, Sintchak Michael D, Smith Michael D, Stroud Stephen G, Tregay Ming, Tian Yuan, Veiby Ole P, Vos Tricia J, Vyskocil Stepan, Williams Juliet, Xu Tianlin, Yang Johnny J, Yano Jason, Zeng Hongbo, Zhang Dong Mei, Zhang Qin, Galvin Katherine M

Abstract excerpt

Inhibition of mutant B-Raf signaling, through either direct inhibition of the enzyme or inhibition of MEK, the direct substrate of Raf, has been demonstrated preclinically to inhibit tumor growth. Very recently, treatment of B-Raf mutant melanoma patients with a selective B-Raf inhibitor has resu...

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PMID: 21341678
DOI: 10.1021/jm101479y

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 4 Sept 2026. Prepared record publication-21341678-2026-09-04.2. Manifest publication-graph-cohort-2026-09-04.2.

Source receipt: PubMed via Helena Literature Corpus, retrieved 4 Sept 2026.

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