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Synthesis and biological evaluation of antitumour-active betulin derivatives
Journal article   Peer reviewed

Synthesis and biological evaluation of antitumour-active betulin derivatives

René Csuk, Alexander Barthel, Ralph Kluge, Dieter Ströhl, Harish Kommera and Reinhard Paschke
Bioorganic & medicinal chemistry, Vol.18(3), pp.1344-1355
01/02/2010
PMID: 20034802

Abstract

Antitumour activity Apoptosis Betulin Betulinic acid
The reaction of betulinic aldehydes with various carbon nucleophiles gave a series of new betulin derivatives, among them epoxides, glycidic derivatives and β-hydroxy carbonyl compounds. Subsequent transformations of the β-hydroxy carbonyls lead to 1,3-diketo- and α,β-unsaturated betulin derivatives. These compounds were assayed for cytotoxicity using 15 human cancer cell lines and a colorimetric SRB-assay. Several compounds revealed significant antitumour activity.

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