PUBLICATION
5-Benzylidene-2,4-thiazolidenedione derivatives: Design, synthesis and evaluation as inhibitors of angiogenesis targeting VEGR-2
- Authors
- Bhanushali, U., Rajendran, S., Sarma, K., Kulkarni, P., Chatti, K., Chatterjee, S., Ramaa, C.S.
- ID
- ZDB-PUB-160709-11
- Date
- 2016
- Source
- Bioorganic chemistry 67: 139-147 (Journal)
- Registered Authors
- Chatti, Kiranam
- Keywords
- 5-Benzylidene-2,4-thiazolidinediones, CAM assay, Docking, VEGFR2, Zebrafish embryo
- MeSH Terms
-
- Animals
- Benzylidene Compounds/chemical synthesis
- Benzylidene Compounds/chemistry
- Benzylidene Compounds/pharmacology*
- Dose-Response Relationship, Drug
- Drug Design*
- Humans
- Molecular Structure
- Neovascularization, Pathologic/drug therapy*
- Neovascularization, Pathologic/pathology
- Protein Kinase Inhibitors/chemical synthesis
- Protein Kinase Inhibitors/chemistry
- Protein Kinase Inhibitors/pharmacology*
- Structure-Activity Relationship
- Thiazoles/chemical synthesis
- Thiazoles/chemistry
- Thiazoles/pharmacology*
- Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors*
- Vascular Endothelial Growth Factor Receptor-2/metabolism
- Zebrafish
- PubMed
- 27388635 Full text @ Bioorg. Chem.
Citation
Bhanushali, U., Rajendran, S., Sarma, K., Kulkarni, P., Chatti, K., Chatterjee, S., Ramaa, C.S. (2016) 5-Benzylidene-2,4-thiazolidenedione derivatives: Design, synthesis and evaluation as inhibitors of angiogenesis targeting VEGR-2. Bioorganic chemistry. 67:139-147.
Abstract
A series of novel 5-benzylidene-2,4-thiazolidinediones were designed as inhibitors of angiogenesis targeting VEGFR-2. In docking study, molecules showed similar way of binding with VEGFR-2 as that of the co-crystallized ligand. Compounds were then synthesized, purified and characterized by spectroscopic techniques. Compounds 3f and 3i were found to be most active in the series showing good inhibition of angiogenesis in both CAM and in zebrafish embryo assays. Compound 3i also exhibited IC50 of 0.5μM against VEGFR-2.
Genes / Markers
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Orthology
Engineered Foreign Genes
Mapping