Peer-reviewed veterinary case report
Parthenolide prodrug LC-1 slows growth of intracranial glioma.
- Journal:
- Bioorganic & medicinal chemistry letters
- Year:
- 2015
- Authors:
- Hexum, Joseph K et al.
- Affiliation:
- Department of Medicinal Chemistry · United States
- Species:
- rodent
Abstract
LC-1 (also known as DMAPT or dimethylamino-parthenolide), a prodrug of parthenolide, was tested for anti-proliferative activity against glioma. LC-1 was found to have low micromolar cytotoxic activity against three glioma cell lines and was also found to be brain penetrant in healthy mice (2.1-3.0 brain-to-plasma ratio). In a syngeneic GL261 murine glioma model, LC-1 slowed tumor growth kinetics and extended the survival time of tumor-bearing mice in comparison to the vehicle control. Consequently, LC-1 represents a promising lead compound for further development as a glioma therapy.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/25978958/