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Your search keyword '"Benjamin M. Brandt"' showing total 2 results
Start Over Author "Benjamin M. Brandt" Topic growth factor receptor
2 results on '"Benjamin M. Brandt"'

1. 2-Hydroxy-4,6-diamino-[1,3,5]triazines: A Novel Class of VEGF-R2 (KDR) Tyrosine Kinase Inhibitors

Author

Carl L. Manthey, Nand Baindur, Ioanna Petrounia, Celine Schalk-Hihi, Naresh Chadha, Christian Andrew Baumann, Heidi Ott, Benjamin M. Brandt, Raymond J. Patch, Mark R. Player, Davoud Asgari, Barry A. Springer, and Theodore E. Carver

Subjects
Umbilical Veins, Angiogenesis, Angiogenesis Inhibitors, Cell Line, Structure-Activity Relationship, Organ Culture Techniques, Growth factor receptor, Drug Discovery, Animals, Combinatorial Chemistry Techniques, Humans, Benzothiazoles, Phosphorylation, Aorta, biology, Triazines, Chemistry, Autophosphorylation, Kinase insert domain receptor, Vascular Endothelial Growth Factor Receptor-2, Capillaries, Rats, Thiazoles, Biochemistry, Enzyme inhibitor, Mitogen-activated protein kinase, cardiovascular system, biology.protein, Molecular Medicine, Endothelium, Vascular, Signal transduction, Tyrosine kinase
Abstract

2-Hydroxy-4,6-diamino-[1,3,5]triazines are described which are a novel class of potent inhibitors of the VEGF-R2 (flk-1/KDR) tyrosine kinase. 4-(Benzothiazol-6-ylamino)-6-(benzyl-isopropyl-amino)-[1,3,5]triazin-2-ol (14d) exhibited low nanomolar potency in the in vitro enzyme inhibition assay (IC(50) = 18 nM) and submicromolar inhibitory activity in a KDR-induced MAP kinase autophosphorylation assay in HUVEC cells (IC(50) = 280 nM), and also demonstrated good in vitro selectivity against a panel of growth factor receptor tyrosine kinases. Further, 14d showed antiangiogenic activity in an aortic ring explant assay by blocking endothelial outgrowths in rat aortas with an IC(50) of 1 microM.

Published
2004
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2. Potent 2'-aminoanilide inhibitors of cFMS as potential anti-inflammatory agents

Author

Nand Baindur, Margery A. Chaikin, Davoud Asgari, Wing S. Cheung, Ioanna Petrounia, Robert R. Donatelli, Taxiarchis Georgiadis, Naresh Chadha, Raymond J. Patch, Mark R. Player, and Benjamin M. Brandt

Subjects
Macrophage colony-stimulating factor, Stereochemistry, medicine.drug_class, Clinical Biochemistry, Anti-Inflammatory Agents, Drug Evaluation, Preclinical, Pharmaceutical Science, Receptor, Macrophage Colony-Stimulating Factor, Biochemistry, Anti-inflammatory, Cell Line, Colony stimulating factor 1 receptor, Inhibitory Concentration 50, Structure-Activity Relationship, Growth factor receptor, Piperidines, Drug Discovery, medicine, Humans, Anilides, Molecular Biology, Protein Kinase Inhibitors, Cell Proliferation, chemistry.chemical_classification, Molecular Structure, Macrophages, Organic Chemistry, In vitro, Enzyme, chemistry, Molecular Medicine, Signal transduction, Tyrosine kinase
Abstract

A series of 2′-aminoanilides have been identified which exhibit potent and selective inhibitory activity against the cFMS tyrosine kinase. Initial SAR studies within this series are described which examine aroyl and amino group substitutions, as well as the introduction of hydrophilic substituents on the benzene core. Compound 47 inhibits the isolated enzyme (IC50 = 0.027 μM) and blocks CSF-1-induced proliferation of bone marrow-derived macrophages (IC50 = 0.11 μM) and as such, serves as a lead candidate for further optimization studies.

Published
2007

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