Search Results - "Tanner, Huw"
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Design and Discovery of N‑(2-Methyl-5′-morpholino-6′-((tetrahydro‑2H‑pyran-4-yl)oxy)-[3,3′-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers
Published in Journal of medicinal chemistry (22-06-2017)“…RAS oncogenes have been implicated in >30% of human cancers, all representing high unmet medical need. The exquisite dependency on CRAF kinase in KRAS mutant…”
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A Versatile Synthesis of Unsymmetrical 3,3′-Bioxindoles: Stereoselective Mukaiyama Aldol Reactions of 2-Siloxyindoles with Isatins
Published in Journal of organic chemistry (21-11-2008)“…A new synthesis of 3,3′-bioxindoles is reported that is well suited for the preparation of unsymmetrical structures. In the key step,…”
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Total Synthesis of Spongistatin 1: A Synthetic Strategy Exploiting Its Latent Pseudo-Symmetry
Published in Angewandte Chemie International Edition (26-08-2005)“…The challenging structure and potent growth inhibition properties against a variety of human cancer cell lines make Spongistatin 1 (1) an exciting target for…”
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Synthesis of the C-1−C-28 ABCD Unit of Spongistatin 1
Published in Organic letters (11-12-2003)“…The synthesis of the C-1−C-28 ABCD fragment of spongistatin is described. Anti-selective boron-mediated aldol coupling of a CD spiroketal ketone fragment to an…”
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A Practical and Efficient Synthesis of the C-16−C-28 Spiroketal Fragment (CD) of the Spongistatins
Published in Organic letters (11-12-2003)“…A practical and efficient route to the CD spiroketal (C-16−C-28) of the spongistatins is reported. Two stereocenters are introduced from chiral building blocks…”
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Design and Discovery of N‑(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the Clinic
Published in Journal of medicinal chemistry (12-03-2020)“…Direct pharmacological inhibition of RAS has remained elusive, and efforts to target CRAF have been challenging due to the complex nature of RAF signaling,…”
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Abstract 330: Development of a highly selective BCRAF kinase inhibitor that exhibits antitumor activities in RAS and BRAF mutant tumors with minimal paradoxical activation
Published in Cancer research (Chicago, Ill.) (15-07-2016)“…The mitogen-activated protein kinase (MAPK) signaling pathway is frequently activated in human cancers due to genetic alterations that can occur at multiple…”
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Abstract 330: Development of a highly selective B/CRAF kinase inhibitor that exhibits antitumor activities in RAS and BRAF mutant tumors with minimal paradoxical activation
Published in Cancer research (Chicago, Ill.) (15-07-2016)“…Abstract The mitogen-activated protein kinase (MAPK) signaling pathway is frequently activated in human cancers due to genetic alterations that can occur at…”
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Total Synthesis of Spongistatin 1: A Synthetic Strategy Exploiting Its Latent Pseudo-Symmetry
Published in Angewandte Chemie (26-08-2005)“…Die komplizierte Struktur und die starke wachstumshemmende Wirkung gegen viele humane Krebszelllinien haben Spongistatin 1 (1) zu einer interessanten…”
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Total Synthesis of Spongistatin 1: A Synthetic Strategy Exploiting Its Latent Pseudo‐Symmetry
Published in Angewandte Chemie (26-08-2005)Get full text
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