2. Academic Validation
  3. Synthesis and biological evaluation of antitumour-active betulin derivatives

Synthesis and biological evaluation of antitumour-active betulin derivatives

  • Bioorg Med Chem. 2010 Feb;18(3):1344-55. doi: 10.1016/j.bmc.2009.12.024.
René Csuk 1,  Alexander Barthel,  Ralph Kluge,  Dieter Ströhl,  Harish Kommera,  Reinhard Paschke
Affiliations

Affiliation

  • 1 Bereich Organische Chemie, Martin-Luther-Universität Halle-Wittenberg, Kurt-Mothes-Str 2, D-06120 Halle, Saale, Germany. rene.csuk@chemie.uni-halle.de
PMID: 20034802 DOI: 10.1016/j.bmc.2009.12.024
Abstract

The reaction of betulinic aldehydes with various carbon nucleophiles gave a series of new betulin derivatives, among them epoxides, glycidic derivatives and beta-hydroxy carbonyl compounds. Subsequent transformations of the beta-hydroxy carbonyls lead to 1,3-diketo- and alpha,beta-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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