Your browser doesn't support javascript.
loading
Parthenolide prodrug LC-1 slows growth of intracranial glioma.
Hexum, Joseph K; Becker, Chani M; Kempema, Aaron M; Ohlfest, John R; Largaespada, David A; Harki, Daniel A.
Afiliação
  • Hexum JK; Department of Medicinal Chemistry, University of Minnesota, Minneapolis, MN 55455, USA.
  • Becker CM; Department of Neuroscience, University of Minnesota, Minneapolis, MN 55455, USA.
  • Kempema AM; Department of Medicinal Chemistry, University of Minnesota, Minneapolis, MN 55455, USA.
  • Ohlfest JR; Department of Pediatrics, University of Minnesota, Minneapolis, MN 55455, USA; Masonic Cancer Center, University of Minnesota, Minneapolis, MN 55455, USA.
  • Largaespada DA; Department of Pediatrics, University of Minnesota, Minneapolis, MN 55455, USA; Masonic Cancer Center, University of Minnesota, Minneapolis, MN 55455, USA.
  • Harki DA; Department of Medicinal Chemistry, University of Minnesota, Minneapolis, MN 55455, USA; Masonic Cancer Center, University of Minnesota, Minneapolis, MN 55455, USA; Stem Cell Institute, University of Minnesota, Minneapolis, MN 55455, USA. Electronic address: daharki@umn.edu.
Bioorg Med Chem Lett ; 25(12): 2493-5, 2015 Jun 15.
Article em En | MEDLINE | ID: mdl-25978958
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.
Assuntos
Palavras-chave
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Sesquiterpenos / Pró-Fármacos Limite: Animals Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2015 Tipo de documento: Article País de afiliação: Estados Unidos
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Sesquiterpenos / Pró-Fármacos Limite: Animals Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2015 Tipo de documento: Article País de afiliação: Estados Unidos