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Your search keyword '"Jean Delgado"' showing total 3 results
Start Over Author "Jean Delgado" Topic drug discovery
3 results on '"Jean Delgado"'

1. 4-Pyridin-5-yl-2-(3,4,5-trimethoxyphenylamino)pyrimidines: Potent and selective inhibitors of ZAP 70

Author

Peter G Davis, Mark James Batchelor, Martin J. Perry, Tom Carabbe, Daniel Berg, Jeremy Martin Davis, O'connell James Philip, Martin Clive Hutchings, David Festus Charles Moffat, James E. Johnson, Jean Delgado, and Richard J. Martin

Subjects
Clinical Biochemistry, Pharmaceutical Science, chemical and pharmacologic phenomena, Biochemistry, Transduction (genetics), Drug Discovery, Phosphorylation, Molecular Biology, chemistry.chemical_classification, ZAP-70 Protein-Tyrosine Kinase, biology, Organic Chemistry, T-cell receptor, hemic and immune systems, Protein-Tyrosine Kinases, In vitro, Cell biology, Pyrimidines, Enzyme, chemistry, Enzyme inhibitor, biology.protein, Molecular Medicine, Signal transduction, Tyrosine kinase, Signal Transduction
Abstract

Activation of the tyrosine kinase ZAP 70 has been shown to be crucial to the transduction of the T-cell receptor signalling pathway, which leads ultimately to proliferation, cytokine gene expression and T-cell effector functions. A series of 2-phenylaminopyrimidines have been identified as potent and selective inhibitors of ZAP 70.

Published
1999
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2. Discovery of 4-azaindoles as novel inhibitors of c-Met kinase

Author

John Robert Porter, Mark James Batchelor, Fabien Lecomte, Christoph Meier, Jean Keyaerts, Lloyd King, Jose M. Gascon-Simorte, James Thomas Reuberson, Alison Maloney, Kelly Le Riche, Jean Delgado, Mark Daniel Calmiano, Bénédicte Lallemand, Simon Lumb, Anne Marie Foley, Richard J. Franklin, and Helen Edwards

Subjects
C-Met, Indoles, Stereochemistry, Clinical Biochemistry, Pharmaceutical Science, Tumor cells, Crystallography, X-Ray, Biochemistry, chemistry.chemical_compound, Structure-Activity Relationship, Growth factor receptor, Cell Line, Tumor, Drug Discovery, Transferase, Humans, Computer Simulation, Molecular Biology, Protein Kinase Inhibitors, chemistry.chemical_classification, Kinase, Organic Chemistry, Proto-Oncogene Proteins c-met, Enzyme, chemistry, Molecular Medicine, Signal transduction
Abstract

A series of 4-azaindole inhibitors of c-Met kinase is described. The postulated binding mode was confirmed by an X-ray crystal structure and series optimisation was performed on the basis of this structure. Future directions for series development are discussed.

Published
2009

3. Discovery of a novel series of quinoxalines as inhibitors of c-Met kinase

Author

Jose M. Gascon-Simorte, Mark Daniel Calmiano, James Thomas Reuberson, John B. Porter, Richard J. Franklin, Helen Edwards, Jean Delgado, Alison Maloney, Kelly Le Riche, Mark James Batchelor, Fabien Lecomte, Christoph Meier, Simon Lumb, and Anne Marie Foley

Subjects
C-Met, Series (mathematics), Drug discovery, Kinase, Stereochemistry, Organic Chemistry, Clinical Biochemistry, Quinoline, Pharmaceutical Science, Proto-Oncogene Proteins c-met, Crystallography, X-Ray, Biochemistry, chemistry.chemical_compound, Structure-Activity Relationship, Quinoxaline, chemistry, Quinoxalines, Drug Discovery, Molecular Medicine, Transferase, Structure–activity relationship, Enzyme Inhibitors, Molecular Biology
Abstract

A series of quinoxaline inhibitors of c-Met kinase is described. The postulated binding mode was confirmed by an X-ray crystal structure and optimisation of the series was performed on the basis of this structure. Future directions for development of the series are discussed together with the identification of a novel quinoline scaffold.

Published
2008

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