PUBLICATION
Tetrahydroquinoline-derived macrocyclic toolbox: the discovery of antiangiogenesis agents in zebrafish assay
- Authors
- Reddy Guduru, S.K., Chamakuri, S., Chandrasekar, G., Kitambi, S.S., Arya, P.
- ID
- ZDB-PUB-140606-4
- Date
- 2013
- Source
- ACS Medicinal Chemistry Letters 4: 666-70 (Journal)
- Registered Authors
- Kitambi, Satish Srinivas
- Keywords
- Natural product-inspired compounds, antiangiogenesis agents, macrocyclic diversity, zebrafish screen
- MeSH Terms
- none
- PubMed
- 24900727 Full text @ ACS Med. Chem. Lett.
Citation
Reddy Guduru, S.K., Chamakuri, S., Chandrasekar, G., Kitambi, S.S., Arya, P. (2013) Tetrahydroquinoline-derived macrocyclic toolbox: the discovery of antiangiogenesis agents in zebrafish assay. ACS Medicinal Chemistry Letters. 4:666-70.
Abstract
A novel approach to incorporate the macrocyclic rings onto the privileged substructure, i.e., tetrahydroquinoline scaffold, is developed. The presence of an amino acid-derived moiety in the macrocyclic skeleton provides an opportunity to modulate the nature of the chiral side chain. Further, evaluation in a zebrafish screen identified three active small molecules (2.5b, 3.2d, and 4.2) as antiangiogenesis agents at 2.5 μM.
Genes / Markers
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Orthology
Engineered Foreign Genes
Mapping