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Your search keyword '"Renhowe PA"' showing total 3 results
Start Over Author "Renhowe PA" Topic raf kinases
3 results on '"Renhowe PA"'

1. Design and synthesis of 6,6-fused heterocyclic amides as raf kinase inhibitors.

Author

Ramurthy S, Costales A, Jansen JM, Levine B, Renhowe PA, Shafer CM, and Subramanian S

Subjects
Amides chemistry, Binding Sites, Cells, Cultured, Enzyme Activation drug effects, Enzyme Inhibitors chemistry, Heterocyclic Compounds chemical synthesis, Heterocyclic Compounds chemistry, Heterocyclic Compounds pharmacology, Humans, Models, Molecular, Molecular Structure, Amides chemical synthesis, Amides pharmacology, Drug Design, Enzyme Inhibitors chemical synthesis, Enzyme Inhibitors pharmacology, raf Kinases antagonists & inhibitors
Abstract

Compounds belonging to several scaffolds-quinazolines, quinolines and quinoxalines-were designed and synthesized as Raf kinase inhibitors. Scaffolds were assessed for in vitro Braf(V600E) inhibition, and overall kinase selectivity. Pharmacokinetic parameters for one of the scaffolds were also determined., (Copyright © 2011 Elsevier Ltd. All rights reserved.)

Published
2012
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2. Design and synthesis of 5,6-fused heterocyclic amides as Raf kinase inhibitors.

Author

Ramurthy S, Aikawa M, Amiri P, Costales A, Hashash A, Jansen JM, Lin S, Ma S, Renhowe PA, Shafer CM, Subramanian S, Sung L, and Verhagen J

Subjects
Amides chemistry, Amides pharmacology, Binding Sites, Cell Proliferation, Enzyme Activation drug effects, Enzyme Inhibitors chemistry, Heterocyclic Compounds chemistry, Heterocyclic Compounds pharmacology, Models, Molecular, Molecular Structure, Structure-Activity Relationship, Amides chemical synthesis, Drug Design, Enzyme Inhibitors chemical synthesis, Enzyme Inhibitors pharmacology, Heterocyclic Compounds chemical synthesis, raf Kinases antagonists & inhibitors
Abstract

Two scaffolds based on 5,6-fused heterocyclic backbones were designed and synthesized as Raf kinase inhibitors. The scaffolds were assessed for in vitro pan-Raf inhibition, activity in cell proliferation and target modulation assays, and pharmacokinetic parameters., (Copyright © 2011. Published by Elsevier Ltd.)

Published
2011
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3. Design and synthesis of orally bioavailable benzimidazoles as Raf kinase inhibitors.

Author

Ramurthy S, Subramanian S, Aikawa M, Amiri P, Costales A, Dove J, Fong S, Jansen JM, Levine B, Ma S, McBride CM, Michaelian J, Pick T, Poon DJ, Girish S, Shafer CM, Stuart D, Sung L, and Renhowe PA

Subjects
Administration, Oral, Animals, Benzimidazoles administration & dosage, Benzimidazoles chemistry, Biological Availability, Cell Line, Tumor, Cell Proliferation drug effects, Crystallography, X-Ray, Dose-Response Relationship, Drug, Female, Humans, Mice, Models, Molecular, Molecular Structure, Protein Kinase Inhibitors administration & dosage, Protein Kinase Inhibitors chemistry, Protein Structure, Tertiary, Stereoisomerism, Structure-Activity Relationship, Xenograft Model Antitumor Assays, raf Kinases metabolism, Benzimidazoles chemical synthesis, Benzimidazoles pharmacology, Drug Design, Protein Kinase Inhibitors chemical synthesis, Protein Kinase Inhibitors pharmacology, raf Kinases antagonists & inhibitors
Abstract

A series of arylaminobenzimidazoles was designed and synthesized as Raf kinase inhibitors. Exploration of the structure-activity relationship resulted in compounds that are potent in vitro and show desirable in vivo properties.

Published
2008
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