期刊
ARCHIV DER PHARMAZIE
卷 344, 期 1, 页码 37-49出版社
WILEY-BLACKWELL
DOI: 10.1002/ardp.201000232
关键词
Antitumor activity; Betulin; Betulinic acid; 1,3-Dipolar-cycloaddition; Liposomes; SRB assay
资金
- Biosolutions Halle GmbH
- Stiftung der Deutschen Wirtschaft (SOW)
Novel betulin derivatives were prepared and tested for their antitumor activity. Starting from 3-O-acetyl- or 3-O-methyl-betulinic aldehyde, the synthesis of C-28 ethynyl derivatives was performed; their subsequent transformation with several 1,3-dipolarophiles afforded pyrazoles and 1,2,3-triazoles. Their screening for antitumor activity was performed in a panel of 15 human cancer cell lines by a colorimetric SRB-assay. Thereby, several compounds revealed a higher cytotoxicity than betulinic acid. In addition, the encapsulation of the lead structure 7 into liposomes was investigated. The results from a dye exclusion test and from DNA laddering experiments provided evidence for an apoptotic cell death.
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