Csuk, RenéSczepek, RonnySiewert, BiankaNitsche, Christoph2025-05-232025-05-230968-0896PubMed:23245801ORCID:/0000-0002-3704-2699/work/162948551http://www.scopus.com/inward/record.url?scp=84871629620&partnerID=8YFLogxKhttps://hdl.handle.net/1885/733753052Several 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.11enAnnexin V assayAntitumorApoptosisBetulinCancerDNA ladderingHydroxypropargylaminesMannich reactionSRB assay2013-01-1510.1016/j.bmc.2012.11.01684871629620