Abstract
Optimization from compound 4a, having intramolecular S-O nonbonded interaction, led to discover compounds 4m and 4n. They were highly active in vitro (VEGF induced HUVEC proliferation assay) and showed efficacies in three disease models in vivo (cancer, RA, AMD).
Copyright © 2010 Elsevier Ltd. All rights reserved.
MeSH terms
-
Anilides / chemical synthesis
-
Anilides / chemistry*
-
Anilides / therapeutic use
-
Animals
-
Arthritis, Experimental / drug therapy
-
Cell Line
-
Choroidal Neovascularization / drug therapy
-
Disease Models, Animal
-
Endothelial Cells / cytology
-
Humans
-
Mice
-
Neoplasms / drug therapy
-
Pyridines / chemical synthesis
-
Pyridines / chemistry*
-
Pyridines / therapeutic use
-
Rats
-
Structure-Activity Relationship
-
Vascular Endothelial Growth Factor A / antagonists & inhibitors*
-
Vascular Endothelial Growth Factor A / metabolism
-
Xenograft Model Antitumor Assays
Substances
-
Anilides
-
Pyridines
-
Vascular Endothelial Growth Factor A
-
pyridine