Search Results - "Rosner, Kristin E."
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Discovery and SAR of hydantoin TACE inhibitors
Published in Bioorganic & medicinal chemistry letters (15-03-2010)“…A novel series of hydantoin TACE inhibitors is disclosed. The initial design and SAR optimization of the series, as well as accompanying X-ray structural and…”
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2
Pyrazolo[1,5- a]pyrimidine-based inhibitors of HCV polymerase
Published in Bioorganic & medicinal chemistry letters (15-11-2009)“…Synthesis and optimization of novel pyrazolo[1,5- a]pyrimidine HCV polymerase inhibitors are described. The present paper describes a novel series of HCV RNA…”
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2-(2-Aminothiazol-4-yl)pyrrolidine-based tartrate diamides as potent, selective and orally bioavailable TACE inhibitors
Published in Bioorganic & medicinal chemistry letters (15-05-2011)“…TNF-α converting enzyme (TACE) inhibitors are promising agents to treat inflammatory disorders and cancer. We have investigated novel tartrate diamide TACE…”
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4
Biaryl substituted hydantoin compounds as TACE inhibitors
Published in Bioorganic & medicinal chemistry letters (01-09-2010)“…A series of biaryl substituted hydantoin TACE inhibitors is disclosed. Many compounds in this series exhibit sub-nanomolar TACE activities and good rat PK. We…”
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5
Discovery of 4H-pyrazolo[1,5-a]pyrimidin-7-ones as potent inhibitors of hepatitis C virus polymerase
Published in Bioorganic & medicinal chemistry letters (15-09-2009)“…A series of 4H-pyrazolo[1,5-a]pyrimidin-7-one derivatives was synthesized and evaluated for inhibitory activity against HCV NS5B RNA-dependent RNA polymerase…”
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6
The discovery of novel tartrate-based TNF-α converting enzyme (TACE) inhibitors
Published in Bioorganic & medicinal chemistry letters (01-02-2010)“…Synthesis and optimization of novel tartrate TACE inhibitors are described. A novel series of TNF-α convertase (TACE) inhibitors which are non-hydroxamate have…”
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Novel TNF-α converting enzyme (TACE) inhibitors as potential treatment for inflammatory diseases
Published in Bioorganic & medicinal chemistry letters (15-12-2010)“…Our research on hydantoin based TNF-α converting enzyme (TACE) inhibitors has led to an acetylene containing series that demonstrates sub-nanomolar potency ( K…”
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8
Structure and activity relationships of tartrate-based TACE inhibitors
Published in Bioorganic & medicinal chemistry letters (15-08-2010)“…The syntheses and structure–activity relationships of the tartrate-based TACE inhibitors are discussed. The optimization of both the prime and non-prime sites…”
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9
The discovery of novel tartrate-based TNF-a converting enzyme (TACE) inhibitors
Published in Bioorganic & medicinal chemistry letters (17-09-2010)“…A novel series of TNF-a convertase (TACE) inhibitors which are non-hydroxamate have been discovered. These compounds are bis-amides of l-tartaric acid…”
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10
Aminothiazole inhibitors of HCV RNA polymerase
Published in Bioorganic & medicinal chemistry letters (03-01-2005)“…[Display omitted] Aminothiazole-based inhibitors designed for HCV polymerase display low micromolar potencies in biochemical assays. These compounds show a…”
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11
An affinity selection–mass spectrometry method for the identification of small molecule ligands from self-encoded combinatorial libraries
Published in International journal of mass spectrometry (01-11-2004)“…The NeoGenesis Automated Ligand Identification System (ALIS), an affinity selection–mass spectrometry (AS–MS) process consisting of a rapid size-exclusion…”
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12
Discovery of 4 H-pyrazolo[1,5- a]pyrimidin-7-ones as potent inhibitors of hepatitis C virus polymerase
Published in Bioorganic & medicinal chemistry letters (2009)“…The design, synthesis and evaluation of a series of 4 H-Pyrazolo[1,5- a]pyrimidin-7-ones as potent inhibitors of hepatitis C virus polymerase are described. A…”
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13
The synthesis of 6,9-bis[(aminoalkyl)amino] substituted benzo[g]quinoxaline-, benzo[g]quinazoline- and benzo-[g]phthalazine-5,10-diones via regiospecific displacements
Published in Journal of heterocyclic chemistry (01-12-1993)“…The synthesis of 6,9‐difluoro substituted benzo[g]quinoxaline‐5,10‐diones (3A), benzo[g]quinazoline‐5,10‐diones (3B) and benzo[g]phthalazine‐5,10‐diones (3C)…”
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