Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 25, Issue 12, Pages 2493-2495Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2015.04.058
Keywords
Blood-brain barrier; Glioblastoma; LC-1; Parthenolide; Pharmacokinetics
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Funding
- Hyundai Hope on Wheels (Hope Grant Award)
- V Foundation for Cancer Research (V Scholar Award)
- Children's Cancer Research Fund (Minneapolis, MN)
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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. (C) 2015 Elsevier Ltd. All rights reserved.
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