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Synthesis and biological evaluation of antitumor-active γ-butyrolactone substituted betulin derivatives
Journal article   Peer reviewed

Synthesis and biological evaluation of antitumor-active γ-butyrolactone substituted betulin derivatives

René Csuk, Alexander Barthel, Stefan Schwarz, Harish Kommera and Reinhard Paschke
Bioorganic & medicinal chemistry, Vol.18(7), pp.2549-2558
01/04/2010
PMID: 20299226

Abstract

Antitumor activity Apoptosis Betulin Betulinic acid γ-Butyrolactone
The plant triterpenes betulin and betulinic acid (BA) are triterpenes featuring interesting pharmacological properties. Starting from substituted betulinic aldehydes, we used them as lead structures for the synthesis of several γ-butyrolactones and butenolides. Their antitumor activity was examined for 15 cancer cell lines using a SRB-assay and their apoptotic action was documented by trypan-blue test and DNA laddering. Several compounds revealed a higher activity than betulinic acid.

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