PUBLICATION
Design, synthesis and evaluation of 5-pyridin-4-yl-2-thioxo-[1,3,4]oxadiazol-3-yl derivatives as anti-angiogenic agents Targeting VEGFR-2
- Authors
- Bhanushali, U., Kalekar-Joshi, S., Kulkarni-Munshi, R., Yellanki, S., Medishetty, R., Kulkarni, P., Ramaa, C.S.
- ID
- ZDB-PUB-160505-6
- Date
- 2017
- Source
- Anti-cancer agents in medicinal chemistry 17(1): 67-74 (Journal)
- Registered Authors
- Kulkarni, Pushkar
- Keywords
- 3-substituted-5-(4-pyridin-4yl)-1, 3, 4-oxadiazole-2-thiones, VEGFR2, Docking, CAM assay, Zebrafish embryo
- MeSH Terms
-
- Angiogenesis Inhibitors/chemical synthesis
- Angiogenesis Inhibitors/chemistry*
- Angiogenesis Inhibitors/pharmacology*
- Animals
- Chickens
- Chorioallantoic Membrane/blood supply
- Chorioallantoic Membrane/drug effects
- Drug Design
- Humans
- Molecular Docking Simulation
- Oxadiazoles/chemical synthesis
- Oxadiazoles/chemistry*
- Oxadiazoles/pharmacology*
- Thiones/chemical synthesis
- Thiones/chemistry
- Thiones/pharmacology
- Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors*
- Vascular Endothelial Growth Factor Receptor-2/metabolism
- Zebrafish/embryology
- PubMed
- 27141880 Full text @ Anticancer Agents Med Chem
Citation
Bhanushali, U., Kalekar-Joshi, S., Kulkarni-Munshi, R., Yellanki, S., Medishetty, R., Kulkarni, P., Ramaa, C.S. (2017) Design, synthesis and evaluation of 5-pyridin-4-yl-2-thioxo-[1,3,4]oxadiazol-3-yl derivatives as anti-angiogenic agents Targeting VEGFR-2. Anti-cancer agents in medicinal chemistry. 17(1):67-74.
Abstract
A series of novel 3-substituted-5-(4-pyridin-4yl)-1,3,4-oxadiazole-2-thiones were designed as inhibitors of angiogenesis targeting VEGFR2. In docking study, all the molecules showed similar way of binding with VEGFR2 as that of the co-crystallised ligand. Compounds were then synthesized, purified and characterized by spectroscopic techniques. Further these Compounds were evaluated for their angiogenesis inhibition potential using CAM and zebrafish assay. Compound 3i and 3j were found to be most active in the series showing good inhibition of angiogenesis in both CAM and in zebrafish embryo assays. The compound 3i was the most active in the series with IC50 of 0.5 μM for VEGR-2.
Genes / Markers
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Orthology
Engineered Foreign Genes
Mapping