PUBLICATION
Identification of noreremophilane-based inhibitors of angiogenesis using zebrafish assays
- Authors
- Muthukumarasamy, K.M., Handore, K.L., Kakade, D.N., Shinde, M.V., Ranjan, S., Kumar, N., Sehrawat, S., Sachidanandan, C., Reddy, D.S.
- ID
- ZDB-PUB-151021-11
- Date
- 2016
- Source
- Organic & biomolecular chemistry 14(5): 1569-78 (Journal)
- Registered Authors
- Keywords
- none
- MeSH Terms
-
- Angiogenesis Inhibitors/chemical synthesis
- Angiogenesis Inhibitors/chemistry
- Angiogenesis Inhibitors/pharmacology*
- Animals
- Embryo, Nonmammalian/blood supply*
- Embryo, Nonmammalian/drug effects*
- Embryo, Nonmammalian/pathology
- Humans
- Molecular Conformation
- Neovascularization, Pathologic/drug therapy*
- Sesquiterpenes/chemical synthesis
- Sesquiterpenes/chemistry
- Sesquiterpenes/pharmacology*
- Xenograft Model Antitumor Assays
- Zebrafish/embryology*
- PubMed
- 26483278 Full text @ Org. Biomol. Chem.
Citation
Muthukumarasamy, K.M., Handore, K.L., Kakade, D.N., Shinde, M.V., Ranjan, S., Kumar, N., Sehrawat, S., Sachidanandan, C., Reddy, D.S. (2016) Identification of noreremophilane-based inhibitors of angiogenesis using zebrafish assays. Organic & biomolecular chemistry. 14(5):1569-78.
Abstract
Noreremophilanes are a rare class of cis-hydrindanes produced by genus Ligularia herbaceous plants which are known to exhibit interesting biological activities. We synthesized cis-hydrindanes based on a naturally occurring noreremophilane scaffold using a Diels-Alder/aldol sequence and screened them for multiple biological activities using high-content zebrafish embryonic development assays. We discovered a noreremophilane that has strong anti-angiogenic effects on the developing zebrafish embryos as well as on tumor-induced angiogenesis in a zebrafish xenograft model. We synthesized several derivatives of this class of noreremophilanes and performed structure-activity relationship studies in zebrafish to identify more potent and less toxic analogs of the original structure.
Genes / Markers
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Orthology
Engineered Foreign Genes
Mapping