Author: "Nelson LT" / Topic: pyridines - Searchworks@Jio Institute Digital Library Search Results

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Start Over Author "Nelson LT" Topic pyridines

Author: Zhao H, Serby MD, Xin Z, Szczepankiewicz BG, Liu M, Kosogof C, Liu B, Nelson LT, Johnson EF, Wang S, Pederson T, Gum RJ, Clampit JE, Haasch DL, Abad-Zapatero C, Fry EH, Rondinone C, Trevillyan JM, Sham HL, and Liu G
Subjects: Administration, Oral, Amides pharmacokinetics, Amides pharmacology, Animals, Biological Availability, Crystallography, X-Ray, Humans, In Vitro Techniques, Mice, Microsomes metabolism, Models, Molecular, Pyridines pharmacokinetics, Pyridines pharmacology, Rats, Structure-Activity Relationship, Thermodynamics, Amides chemical synthesis, JNK Mitogen-Activated Protein Kinases antagonists & inhibitors, Pyridines chemical synthesis
Abstract: C-Jun NH2 terminal kinases (JNKs) are important cell signaling enzymes. JNK1 plays a central role in linking obesity and insulin resistance. JNK2 and JNK3 may be involved in inflammatory and neurological disorders, respectively. Small-molecule JNK inhibitors could be valuable tools to study the therapeutic benefits of inhibiting these enzymes and as leads for potential drugs targeting JNKs. In this report, we disclose a series of potent and highly selective JNK inhibitors with good pharmacokinetic profiles.
Published: 2006
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Author: Gwaltney SL 2nd, O'Connor SJ, Nelson LT, Sullivan GM, Imade H, Wang W, Hasvold L, Li Q, Cohen J, Gu WZ, Tahir SK, Bauch J, Marsh K, Ng SC, Frost DJ, Zhang H, Muchmore S, Jakob CG, Stoll V, Hutchins C, Rosenberg SH, and Sham HL
Subjects: Biological Availability, Crystallography, X-Ray, Enzyme Inhibitors pharmacokinetics, Farnesyltranstransferase, Genes, ras drug effects, Glycine pharmacology, Histidine pharmacology, Models, Molecular, Molecular Conformation, Phenylalanine pharmacology, Structure-Activity Relationship, Alkyl and Aryl Transferases antagonists & inhibitors, Enzyme Inhibitors chemical synthesis, Enzyme Inhibitors pharmacology, Glycine analogs & derivatives, Histidine analogs & derivatives, Phenylalanine analogs & derivatives, Pyridines chemical synthesis, Pyridines pharmacology
Abstract: Inhibitors of farnesyltransferase are effective against a variety of tumors in mouse models of cancer. Clinical trials to evaluate these agents in humans are ongoing. In our effort to develop new farnesyltransferase inhibitors, we have discovered a series of aryl tetrahydropyridines that incorporate substituted glycine, phenylalanine and histidine residues. The design, synthesis, SAR and biological properties of these compounds will be discussed.
Published: 2003
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Author: Gwaltney SL 2nd, O'Connor SJ, Nelson LT, Sullivan GM, Imade H, Wang W, Hasvold L, Li Q, Cohen J, Gu WZ, Tahir SK, Bauch J, Marsh K, Ng SC, Frost DJ, Zhang H, Muchmore S, Jakob CG, Stoll V, Hutchins C, Rosenberg SH, and Sham HL
Subjects: Alkylation, Animals, Biological Availability, Dogs, Enzyme Inhibitors pharmacokinetics, Farnesyltranstransferase, Half-Life, Models, Molecular, Pyridines pharmacokinetics, Structure-Activity Relationship, Alkyl and Aryl Transferases antagonists & inhibitors, Enzyme Inhibitors chemical synthesis, Enzyme Inhibitors pharmacology, Pyridines chemical synthesis, Pyridines pharmacology
Abstract: Inhibitors of farnesyltransferase are effective against a variety of tumors in mouse models of cancer. Clinical trials to evaluate these agents in humans are ongoing. In our effort to develop new farnesyltransferase inhibitors, we have discovered bioavailable aryl tetrahydropyridines that are potent in cell culture. The design, synthesis, SAR and biological properties of these compounds will be discussed.
Published: 2003
Full Text: View/download PDF

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