Search Results - "Renhowe, Paul"
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Discovery of stimulator binding to a conserved pocket in the heme domain of soluble guanylyl cyclase
Published in The Journal of biological chemistry (02-02-2018)“…Soluble guanylyl cyclase (sGC) is the receptor for nitric oxide and a highly sought-after therapeutic target for the management of cardiovascular diseases. New…”
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Solution structures of the Shewanella woodyi H‐NOX protein in the presence and absence of soluble guanylyl cyclase stimulator IWP‐051
Published in Protein science (01-02-2021)“…Heme‐nitric oxide/oxygen binding (H‐NOX) domains bind gaseous ligands for signal transduction in organisms spanning prokaryotic and eukaryotic kingdoms. In the…”
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3
Synthesis, Binding Mode, and Antihyperglycemic Activity of Potent and Selective (5-Imidazol-2-yl-4-phenylpyrimidin-2-yl)[2-(2-pyridylamino)ethyl]amine Inhibitors of Glycogen Synthase Kinase 3
Published in Journal of medicinal chemistry (26-10-2017)“…In an effort to identify new antidiabetic agents, we have discovered a novel family of…”
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The CNS-Penetrant Soluble Guanylate Cyclase Stimulator CY6463 Reveals its Therapeutic Potential in Neurodegenerative Diseases
Published in Frontiers in pharmacology (24-05-2021)“…Effective treatments for neurodegenerative diseases remain elusive and are critically needed since the burden of these diseases increases across an aging…”
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Discovery of CYR715: A novel carboxylic acid-containing soluble guanylate cyclase stimulator
Published in Bioorganic & medicinal chemistry letters (15-05-2021)“…[Display omitted] Soluble guanylate cyclase (sGC) is a clinically validated therapeutic target in the treatment of pulmonary hypertension. Modulators of sGC…”
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Design, Structure−Activity Relationships and in Vivo Characterization of 4-Amino-3-benzimidazol-2-ylhydroquinolin-2-ones: A Novel Class of Receptor Tyrosine Kinase Inhibitors
Published in Journal of medicinal chemistry (22-01-2009)“…The inhibition of key receptor tyrosine kinases (RTKs) that are implicated in tumor vasculature formation and maintenance, as well as tumor progression and…”
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Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma
Published in ACS medicinal chemistry letters (10-09-2015)“…Abrogation of errant signaling along the MAPK pathway through the inhibition of B-RAF kinase is a validated approach for the treatment of pathway-dependent…”
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8
Design and Synthesis of Orally Bioavailable Benzimidazoles as Raf Kinase Inhibitors
Published in Journal of medicinal chemistry (27-11-2008)“…A series of arylaminobenzimidazoles was designed and synthesized as Raf kinase inhibitors. Exploration of the structure−activity relationship resulted in…”
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Design and synthesis of 6,6-fused heterocyclic amides as raf kinase inhibitors
Published in Bioorganic & medicinal chemistry letters (15-02-2012)“…Compounds belonging to several scaffolds—quinazolines, quinolines and quinoxalines—were designed and synthesized as Raf kinase inhibitors. Scaffolds were…”
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Design and synthesis of 5,6-fused heterocyclic amides as Raf kinase inhibitors
Published in Bioorganic & medicinal chemistry letters (01-06-2011)“…Two scaffolds based on 5,6-fused heterocyclic backbones were designed and synthesized as Raf kinase inhibitors. The scaffolds were assessed for in vitro…”
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Design and Synthesis of Orally Bioavailable Benzimidazole Reverse Amides as Pan RAF Kinase Inhibitors
Published in ACS medicinal chemistry letters (11-09-2014)“…Benzimidazole reverse amides were designed and synthesized as Pan RAF kinase inhibitors. Investigation of the structure–activity relationship of the compounds…”
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Identification and structure–activity relationship of 2-morpholino 6-(3-hydroxyphenyl) pyrimidines, a class of potent and selective PI3 kinase inhibitors
Published in Bioorganic & medicinal chemistry letters (01-12-2010)“…PI3 Kinases are a family of lipid kinases mediating numerous cell processes such as proliferation, migration, and differentiation. The PI3 kinase pathway is…”
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4-(Aminoalkylamino)-3-benzimidazole-quinolinones as potent CHK-1 inhibitors
Published in Bioorganic & medicinal chemistry letters (15-06-2006)“…CHK-1 is one of the key enzymes regulating checkpoints in cellular growth cycles. Novel 4-(amino-alkylamino)-3-benzimidazole-quinolinones were prepared and…”
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Design and structure–activity relationship of 3-benzimidazol-2-yl-1H-indazoles as inhibitors of receptor tyrosine kinases
Published in Bioorganic & medicinal chemistry letters (01-07-2006)“…The synthesis and SAR of 3-benzimidazol-2-yl-1H-indazole analogs developed as inhibitors of receptor tyrosine kinases (RTK) is reported…”
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Enantioselective Total Synthesis of (-)-Ptilomycalin A
Published in Journal of the American Chemical Society (01-03-1995)Get full text
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Correction to Design and Synthesis of Orally Bioavailable Benzimidazole Reverse Amides as Pan RAF Kinase Inhibitors
Published in ACS medicinal chemistry letters (11-12-2014)“…[This corrects the article DOI: 10.1021/ml5002272.]…”
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A Practical Entry to the Crambescidin Family of Guanidine Alkaloids. Enantioselective Total Syntheses of Ptilomycalin A, Crambescidin 657 and Its Methyl Ester (Neofolitispates 2), and Crambescidin 800
Published in Journal of the American Chemical Society (24-05-2000)“…Among the most structurally remarkable guanidine natural products are the crambescidin/ptilomycalin A family of marine alkaloids. The evolution of a practical…”
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3-Benzimidazol-2-yl-1H-indazoles as potent c-ABL inhibitors
Published in Bioorganic & medicinal chemistry letters (15-07-2006)“…The 3-benzimidazol-2-yl-1H-indazole scaffold was developed as an alternate scaffold for our receptor tyrosine kinase (RTK) inhibitor program. In exploring the…”
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Total Synthesis of (+)-Isolaurepinnacin. Use of Acetal-Alkene Cyclizations To Prepare Highly Functionalized Seven-Membered Cyclic Ethers
Published in Journal of the American Chemical Society (12-03-1997)“…The first synthesis of the title compound is described. The synthesis features an acetal-vinylsilane cyclization to stereoselectively form the…”
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Investigations of a Nucleophilic Alaninol Synthon Derived from Serine
Published in Journal of the American Chemical Society (25-08-1999)“…A nucleophilic synthon, (S)-(+)-4-(2-oxazolidonyl)-methyltriphenylphosphinyl iodide 6, available from l-serine in five steps (overall yield of 52%), reacts…”
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