title: Cytotoxic betulin-derived hydroxypropargylamines trigger apoptosis.
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.
authors.affiliation: Bereich Organische Chemie, Martin-Luther-Universität Halle-Wittenberg, Kurt-Mothes-Str. 2, D-06120 Halle (Saale), Germany. rene.csuk@chemie.uni-halle.de
authors.forename: René
authors.initials: R
authors.lastname: Csuk
authors.forename: Ronny
authors.initials: R
authors.lastname: Sczepek
authors.forename: Bianka
authors.initials: B
authors.lastname: Siewert
authors.forename: Christoph
authors.initials: C
authors.lastname: Nitsche
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000633:toxicity*; D017209:Apoptosis / Q000187:drug effects*; D002460:Cell Line; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D061986:MCF-7 Cells; D051379:Mice; D041681:NIH 3T3 Cells; D010293:Pargyline / Q000031:analogs & derivatives* / Q000737:chemistry; D011437:Propylamines / Q000737:chemistry*; D014315:Triterpenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D000094062:Betulinic Acid
chemical_list: D000970:Antineoplastic Agents; D010293:Pargyline; D011437:Propylamines; D014315:Triterpenes; C009054:propargylamine; C002503:betulin; D000094062:Betulinic Acid