Parthenolide prodrug LC-1 slows growth of intracranial glioma
Joseph K Hexum1, Chani M Becker2, Aaron M Kempema1
1Department of Medicinal Chemistry, University of Minnesota, Minneapolis, MN 55455, USA.
Bioorganic & Medicinal Chemistry Letters
|May 17, 2015
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.
