Search Results - "Randolph, Nikole"
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Pyrazolopyridine Inhibitors of B-RafV600E. Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors
Published in ACS medicinal chemistry letters (08-03-2011)“…The V600E mutation of B-Raf kinase results in constitutive activation of the MAPK signaling pathway and is present in approximately 7% of all cancers. Using…”
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Non-oxime pyrazole based inhibitors of B-Raf kinase
Published in Bioorganic & medicinal chemistry letters (01-06-2011)“…The synthesis and biological evaluation of non-oxime pyrazole based B-Raf inhibitors is reported. Several oxime replacements have been prepared and have shown…”
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3
Potent and selective pyrazole-based inhibitors of B-Raf kinase
Published in Bioorganic & medicinal chemistry (15-08-2008)“…We report herein a series of substituted pyrazoles as inhibitors of B-Raf kinase. Through structure–activity relationship studies, cellular potency,…”
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4
Non-oxime inhibitors of B-Raf(V600E) kinase
Published in Bioorganic & medicinal chemistry letters (15-02-2011)“…The development of inhibitors of B-Raf(V600E) serine-threonine kinase is described. Various head-groups were examined to optimize inhibitor activity and ADME…”
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The Discovery of furo[2,3- c]pyridine-based indanone oximes as potent and selective B-Raf inhibitors
Published in Bioorganic & medicinal chemistry letters (15-02-2011)“…Virtual and high-throughput screening identified imidazo[1,2- a]pyrazines as inhibitors of B-Raf. We describe the rationale, SAR, and evolution of the initial…”
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Pyrazolopyridine Inhibitors of B-Raf(V600E). Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors
Published in ACS medicinal chemistry letters (12-05-2011)“…The V600E mutation of B-Raf kinase results in constitutive activation of the MAPK signaling pathway and is present in approximately 7% of all cancers. Using…”
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7
Non-oxime inhibitors of B-Raf super(V600E) kinase
Published in Bioorganic & medicinal chemistry letters (15-02-2011)“…The development of inhibitors of B-Raf super(V600E) serine-threonine kinase is described. Various head-groups were examined to optimize inhibitor activity and…”
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8
Non-oxime inhibitors of B-Raf V600E kinase
Published in Bioorganic & medicinal chemistry letters (2011)“…Inhibitors of B-Raf V600E kinase are reported for which indanone oximes are replaced with tricyclic pyrazoles and indazoles. The development of inhibitors of…”
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Abstract B254: Extended target-coverage by selective Chk1 inhibitors enhances pharmacodynamic inhibition of Chk1 signaling and antitumor activity in vivo
Published in Molecular cancer therapeutics (10-12-2009)“…Abstract Loss of coordination between cell cycle checkpoints and DNA damage repair is a fundamental feature tumor cells rely on for unregulated growth and…”
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Non-oxime inhibitors of B-Rafⱽ⁶⁰⁰ᴱ kinase
Published in Bioorganic & medicinal chemistry letters (01-02-2011)“…The development of inhibitors of B-Rafⱽ⁶⁰⁰ᴱ serine–threonine kinase is described. Various head-groups were examined to optimize inhibitor activity and ADME…”
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11
Pyrazolopyridine Inhibitors of B-Raf V600E . Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors
Published in ACS medicinal chemistry letters (12-05-2011)Get full text
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