Search Results - "Markworth, Christopher J."
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One-Pot Synthesis of Symmetrical and Unsymmetrical Bisarylethynes by a Modification of the Sonogashira Coupling Reaction
Published in Organic letters (19-09-2002)“…A modification of the Sonogoshira coupling reaction employing an amidine base and a substoichiometric amount of water generates symmetrical and unsymmetrical…”
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Discovery of Clinical Candidate 4‑[2-(5-Amino‑1H‑pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro‑N‑1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of NaV1.7
Published in Journal of medicinal chemistry (24-08-2017)“…A series of acidic diaryl ether heterocyclic sulfonamides that are potent and subtype selective NaV1.7 inhibitors is described. Optimization of early lead…”
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Discovery of Novel 2-Aminobenzamide Inhibitors of Heat Shock Protein 90 as Potent, Selective and Orally Active Antitumor Agents
Published in Journal of medicinal chemistry (23-07-2009)“…A novel class of heat shock protein 90 (Hsp90) inhibitors was developed from an unbiased screen to identify protein targets for a diverse compound library…”
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Discovery of Clinical Candidate 4-[2-(5-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of Na V 1.7
Published in Journal of medicinal chemistry (24-08-2017)“…A series of acidic diaryl ether heterocyclic sulfonamides that are potent and subtype selective Na 1.7 inhibitors is described. Optimization of early lead…”
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5
Discovery of novel aminoquinazolin-7-yl 6,7-dihydro-indol-4-ones as potent, selective inhibitors of heat shock protein 90
Published in Bioorganic & medicinal chemistry letters (01-04-2012)“…Compound affinity to Hsp90 in Kd and cellular activities in IC50. A novel class of Hsp90 inhibitors, structurally distinct from previously reported scaffolds,…”
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Isotope or mass encoding of combinatorial libraries
Published in Chemistry & biology (01-08-1996)“…Background: Combinatorial chemistry using solid-phase synthesis is a rapidly developing technology that can result in a significant reduction in the time…”
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Selective deprotection of alkyl t-butyldimethylsilyl ethers in the presence of aryl t-butyldimethylsilyl ethers
Published in Tetrahedron letters (22-01-1999)“…Alkyl TBS ethers can be selectively cleaved in high yield in the presence of aryl TBS ethers employing either in situ generated hydrogen chloride or hydrogen…”
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Inhibition of potato polyphenol oxidase by anions and activity in various carboxylate buffers (pH 4.8) at constant ionic strength
Published in Journal of enzyme inhibition (2001)“…The activity of potato polyphenol oxidase (tyrosinase) toward DL-3,4-dihydroxyphenylalanine (K(M) 5.39 mM) was studied using a variety of carboxylate buffers…”
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