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Cytotoxic betulin-derived hydroxypropargylamines trigger apoptosis

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2013-01-15

Authors

Csuk, René
Sczepek, Ronny
Siewert, Bianka
Nitsche, Christoph

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Abstract

Several novel betulin derivatives were prepared and evaluated for their antitumor activity. Among others, 3-O-acetylbetulinic aldehyde served as an ideal starting material for the synthesis of 28-acetylenic derivatives that were further transformed into Mannich bases. These hydroxypropargylamines were screened for their antitumor activity in a panel of nine human cancer cell lines in a sulforhodamine B (SRB) assay. Several compounds showed a noteworthy antitumor activity. The results from acridine orange/propidium iodide staining and annexinV-FITC assays as well as DNA laddering experiments provided evidence for an apoptotic cell death.

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Keywords

Annexin V assay, Antitumor, Apoptosis, Betulin, Cancer, DNA laddering, Hydroxypropargylamines, Mannich reaction, SRB assay

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http://www.scopus.com/inward/record.url?scp=84871629620&partnerID=8YFLogxK
 https://hdl.handle.net/1885/733753052

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ANU Research Publications

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Bioorganic and Medicinal Chemistry

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Journal article

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DOI

10.1016/j.bmc.2012.11.016

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