Parthenolide prodrug LC-1 slows growth of intracranial glioma

Joseph K. Hexum, Chani M. Becker, Aaron M. Kempema, John R. Ohlfest, David A. Largaespada, Daniel A. Harki

Research output: Contribution to journalArticlepeer-review

14 Scopus citations

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 languageEnglish (US)
Article number22641
Pages (from-to)2493-2495
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume25
Issue number12
DOIs
StatePublished - 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

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