Synthesis and biological evaluation of antitumour-active betulin derivatives |
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Authors: | René Csuk Alexander Barthel Ralph Kluge Dieter Ströhl Harish Kommera Reinhard Paschke |
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Affiliation: | 1. Bereich Organische Chemie, Martin-Luther-Universität Halle-Wittenberg, Kurt-Mothes-Str. 2, D-06120 Halle, Saale, Germany;2. BioSolutions GmbH, Weinbergweg 22, D-06120 Halle, Saale, Germany |
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Abstract: | 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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