Search Results - "Higley, C. Anne"
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Synthesis and Evaluation of Indenopyrazoles as Cyclin-Dependent Kinase Inhibitors. 3. Structure Activity Relationships at C3
Published in Journal of medicinal chemistry (21-11-2002)“…The identification of indeno[1,2-c]pyrazol-4-ones as inhibitors of cyclin-dependent kinases (CDKs) has led to the discovery of a series of novel and potent…”
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2
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. Part 4: Heterocycles at C3
Published in Bioorganic & medicinal chemistry letters (19-01-2004)“…New indeno[1,2- c]pyrazol-4-one cyclin dependent kinase inhibitors have been disclosed. The most promising compounds are nanomolar enzyme inhibitors with…”
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3
Pyrazoles, 1,2,4-triazoles, and tetrazoles as surrogates for cis-amide bonds in boronate ester thrombin inhibitors
Published in Bioorganic & medicinal chemistry letters (07-04-1998)“…Substituted pyrazoles, 1,2,4-triazoles, and tetrazoles are good surrogates for cis-amide bonds in a series of boronate ester thrombin inhibitors. Substituted…”
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4
MEK inhibitors: The chemistry and biological activity of U0126, its analogs, and cyclization products
Published in Bioorganic & medicinal chemistry letters (20-10-1998)“…In search of antiinflammatory drugs with a new mechanism of action, U0126 was found to functionally antagonize AP-1 transcriptional activity via noncompetitive…”
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5
Discovery of an Orally Active Series of Isoxazoline Glycoprotein IIb/IIIa Antagonists
Published in Journal of medicinal chemistry (20-06-1997)“…Using isoxazoline XR299 (1a) as a starting point for the design of highly potent, long-duration GPIIb/IIIa antagonists, the effect of placing lipophilic…”
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Acyl CoA:Cholesterol Acyltransferase (ACAT) Inhibitors: Synthesis and Structure-Activity Relationship Studies of a New Series of Trisubstituted Imidazoles
Published in Journal of medicinal chemistry (01-10-1994)“…A series of 4,5-diaryl-2-(substituted thio)-1H-imidazoles has been synthesized and demonstrated to be potent inhibitors of acyl-CoA:cholesterol acyltransferase…”
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7
Design, Synthesis, and Structure-Activity Relationship Studies for a New Imidazole Series of J774 Macrophage Specific Acyl-CoA:Cholesterol Acyltransferase (ACAT) Inhibitors
Published in Journal of medicinal chemistry (01-03-1995)“…Acyl-CoA:cholesterol acyltransferase (ACAT) is the primary enzyme involved in intracellular cholesterol esterification. Arterial wall infiltration by…”
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Acyl CoA:cholesterol acyltransferase (ACAT) inhibitors: ureas bearing heterocyclic groups bioisosteric for an imidazole
Published in Bioorganic & medicinal chemistry letters (01-01-1995)“…A series of compounds bearing heterocyclic substituents were prepared, and evaluated for inhibition of the ACAT enzyme. The heterocyclic groups were compared…”
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