Betulinic acid and Glycyrrhetinic acid are of great interest in pharmacological and chemical research because of their great potential for treating several diseases including HIV, herpes and cancer. Both triterpenes are wide-spread in plant kingdom and showed cytotoxic activity against several cancer cell lines by triggering apoptosis. Betulinic acid showed a selective cytotoxicitiy for melanoma cells in an animal model. Because of no acute or chronic side effects even at doses of 500 mg/kg, betulinic acid prevails as a potent alternative in chemotherapeutic therapy, which is currently researched in clinical trials. The subject of this work is synthesis and evaluation of novel derivates of betulinic acid and glycyrrhetinic acid bearing a carbon-carbon triple bond. The prepared alkynol and alkynketone derivates were evaluated by using a SRB assay. Several alkyne derivates showed increased cytotoxic behavior against nine cancer cell lines with IC50 > 1 μM. Additional several triazols and propargyl amines were gained from alkynyl derivates and showed good cytotoxic activity. Further assays like AO/EP, trypan blue, annixin-V , investigation of cell cycle and DNA laddering experiments suggest that alkynyl derivates trigger apoptosis in cancer cell lines.