Search Results - "Fung, Steven"
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Hepatic glucocorticoid receptor antagonism is sufficient to reduce elevated hepatic glucose output and improve glucose control in animal models of type 2 diabetes
Published in The Journal of pharmacology and experimental therapeutics (01-07-2005)“…Glucocorticoids amplify endogenous glucose production in type 2 diabetes by increasing hepatic glucose output. Systemic glucocorticoid blockade lowers glucose…”
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Liver-Selective Glucocorticoid Antagonists: A Novel Treatment for Type 2 Diabetes
Published in Journal of medicinal chemistry (12-08-2004)“…Hepatic blockade of glucocorticoid receptors (GR) suppresses glucose production and thus decreases circulating glucose levels, but systemic glucocorticoid…”
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The synthesis of oligonucleotides containing an aliphatic amino group at the 5′ terminus: synthesis of fluorescent DNA primers for use in DNA sequence analysis
Published in Nucleic acids research (11-04-1985)“…A rapid and versatile method has been developed for the synthesis of oligonucleotides which contain an aliphatic amino group at their 5′ terminus. This amino…”
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Discovery and Metabolic Stabilization of Potent and Selective 2-Amino-N-(adamant-2-yl) Acetamide 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors
Published in Journal of medicinal chemistry (11-01-2007)“…Starting from a rapidly metabolized adamantane 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor 22a, a series of E-5-hydroxy-2-adamantamine…”
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Stereoselective synthesis of brassinolide: a plant growth promoting steroidal lactone
Published in Journal of the American Chemical Society (01-10-1980)Get full text
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Adamantane sulfone and sulfonamide 11-β-HSD1 Inhibitors
Published in Bioorganic & medicinal chemistry letters (15-01-2007)“…The synthesis of potent and selective adamantane sulfone and sulfonamide 11-β-HSD-1 inhibitors represented by 10 and 40 is reported. Potent and selective…”
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Adamantane 11-β-HSD-1 inhibitors: Application of an isocyanide multicomponent reaction
Published in Bioorganic & medicinal chemistry letters (01-12-2006)“…The synthesis of the potent and selective h-11-β-HSD-1 inhibitor 11 ( K i = 8 nm) is reported. A series of potent and selective adamantane aminoamide…”
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Synthesis and structural activity relationship of 11β-HSD1 inhibitors with novel adamantane replacements
Published in Bioorganic & medicinal chemistry letters (15-10-2006)“…A series of structurally novel and metabolically stable bridged bicyclic carbocycle and heterocycle adamantane replacements have been synthesized and…”
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Discovery of adamantane ethers as inhibitors of 11β-HSD-1: Synthesis and biological evaluation
Published in Bioorganic & medicinal chemistry letters (01-02-2007)“…The synthesis and SAR of adamantane ethers are described as novel, potent and selective inhibitors of 11β-HSD-1. An X-ray crystal structure of one of these…”
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Synthesis and biological evaluation of heterocycle containing adamantane 11β-HSD1 inhibitors
Published in Bioorganic & medicinal chemistry letters (15-10-2006)“…A series of metabolically stable adamantane amide 11β-HSD1 inhibitors have been synthesized and biologically evaluated. These compounds exhibit excellent HSD1…”
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Discovery of potent and selective inhibitors of 11β-HSD1 for the treatment of metabolic syndrome
Published in Bioorganic & medicinal chemistry letters (15-12-2006)“…High throughput screening efforts have identified a novel class of dichloroaniline amide 11β-HSD1 inhibitors. SAR studies initiated from dichloroaniline 4…”
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Discovery of orally active butyrolactam 11β-HSD1 inhibitors
Published in Bioorganic & medicinal chemistry letters (01-11-2006)“…A series of metabolically stable butyrolactam 11β-HSD1 inhibitors have been synthesized and biologically evaluated. A series of metabolically stable…”
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Antidiabetic Activity of Passive Nonsteroidal Glucocorticoid Receptor Modulators
Published in Journal of medicinal chemistry (11-08-2005)“…Much has been learned about the consequences of glucocorticoid receptor antagonism by studying steroidal active antagonists such as RU-38486 (1). In the liver…”
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Parallel strategies for the preparation and selection of liver-targeted glucocorticoid receptor antagonists
Published in Bioorganic & medicinal chemistry letters (2007)“…Libraries of mifepristone analogs, MP-Acids, were shown to be potent GR antagonists in binding and cell-based functional screens. A high-throughput…”
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Discovery of potent and selective inhibitors of 11beta-HSD1 for the treatment of metabolic syndrome
Published in Bioorganic & medicinal chemistry letters (15-12-2006)“…High throughput screening efforts have identified a novel class of dichloroaniline amide 11beta-HSD1 inhibitors. SAR studies initiated from dichloroaniline 4…”
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Synthesis and structural activity relationship of 11beta-HSD1 inhibitors with novel adamantane replacements
Published in Bioorganic & medicinal chemistry letters (15-10-2006)“…A series of structurally novel and metabolically stable bridged bicyclic carbocycle and heterocycle adamantane replacements have been synthesized and…”
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Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists
Published in Bioorganic & medicinal chemistry letters (01-12-2006)“…A series of potent steroidal glucocorticoid receptor antagonists has been discovered. After conjugation to cholic acid, the compounds retained an affinity for…”
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Discovery of orally active butyrolactam 11beta-HSD1 inhibitors
Published in Bioorganic & medicinal chemistry letters (01-11-2006)“…A series of metabolically stable butyrolactam 11beta-HSD1 inhibitors have been synthesized and biologically evaluated. These compounds exhibit excellent HSD1…”
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Synthesis and biological evaluation of heterocycle containing adamantane 11beta-HSD1 inhibitors
Published in Bioorganic & medicinal chemistry letters (15-10-2006)“…A series of metabolically stable adamantane amide 11beta-HSD1 inhibitors have been synthesized and biologically evaluated. These compounds exhibit excellent…”
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