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.
Original language | English (US) |
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Article number | 22641 |
Pages (from-to) | 2493-2495 |
Number of pages | 3 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 25 |
Issue number | 12 |
DOIs | |
State | Published - May 26 2015 |
Bibliographical note
Funding Information:We gratefully acknowledge Hyundai Hope on Wheels (Hope Grant Award), The V Foundation for Cancer Research (V Scholar Award to DAH), and the Children’s Cancer Research Fund (Minneapolis, MN) for financial support.
Keywords
- Blood-brain barrier
- Glioblastoma
- LC-1
- Parthenolide
- Pharmacokinetics