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Your search keyword '"Cunningham AM"' showing total 2 results
Start Over Author "Cunningham AM" Journal bioorganic medicinal chemistry letters
2 results on '"Cunningham AM"'

1. Discovery and evaluation of 3-(5-thien-3-ylpyridin-3-yl)-1H-indoles as a novel class of KDR kinase inhibitors.

Author

Fraley ME, Arrington KL, Hambaugh SR, Hoffman WF, Cunningham AM, Young MB, Hungate RW, Tebben AJ, Rutledge RZ, Kendall RL, Huckle WR, McFall RC, Coll KE, and Thomas KA

Subjects
Administration, Oral, Angiogenesis Inhibitors pharmacokinetics, Angiogenesis Inhibitors pharmacology, Animals, Biological Availability, Cell Line, Half-Life, Indoles pharmacology, Inhibitory Concentration 50, Rats, Structure-Activity Relationship, Angiogenesis Inhibitors chemical synthesis, Indoles chemical synthesis, Indoles pharmacokinetics, Vascular Endothelial Growth Factor Receptor-2 antagonists & inhibitors
Abstract

We have discovered 3-(5-thien-3-ylpyridin-3-yl)-1H-indoles as potent inhibitors of KDR kinase activity. This communication details the evolution of this novel class from a potent screening lead of vastly different structure with an emphasis on structural modifications that retained activity and provided improvements in key physical properties. The synthesis and in-depth evaluation of these inhibitors are described.

Published
2003
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2. Design and synthesis of 1,5-diarylbenzimidazoles as inhibitors of the VEGF-receptor KDR.

Author

Bilodeau MT, Cunningham AM, Koester TJ, Ciecko PA, Coll KE, Huckle WR, Hungate RW, Kendall RL, McFall RC, Mao X, Rutledge RZ, and Thomas KA

Subjects
Animals, Chemical Phenomena, Chemistry, Physical, Dogs, Drug Design, Enzyme Inhibitors pharmacokinetics, Half-Life, Hydrogen-Ion Concentration, Indicators and Reagents, Molecular Conformation, Rats, Structure-Activity Relationship, Benzimidazoles chemical synthesis, Benzimidazoles pharmacology, Enzyme Inhibitors chemical synthesis, Enzyme Inhibitors pharmacology, Vascular Endothelial Growth Factor Receptor-2 antagonists & inhibitors
Abstract

1,5-Diarylbenzimidazoles have been identified as potent inhibitors of KDR kinase activity. The series was developed with a goal of finding compounds with optimal drug-like properties. This communication describes structural modifications in the series that enhance solubility, lower protein binding, and provide compounds with excellent potency and pharmacokinetic profiles.

Published
2003
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