New acetylenic derivatives of betulin and betulone, synthesis and cytotoxic activity.
Betulin 1 and its semisynthetic derivatives exhibit a cytotoxic activity toward various cancer cell lines. These compounds are a promising and potential anticancer candidates. A series of betulin derivatives was prepared and tested for the antiproliferative activity in vitro against T47D breast cancer, CCRF/CEM leukemia, HL-60 promyelocytic leukemia, SW707 colorectal, murine P388 leukemia, as well as BALB3T3 normal fibroblasts cell lines. Cisplatin and betulin 1 were used as a reference compounds. Some derivatives of betulin showed a higher cytotoxic activity than the parent compound 1. Two derivatives (5 and 17) were 24-fold potent than betulin 1 against the human promyelocytic leukemia cell line (HL-60), with an IC50 value of 0.3 µg/mL.
['Bębenek|Ewa|E|', 'Kadela-Tomanek|Monika|M|', 'Chrobak|Elwira|E|', 'Wietrzyk|Joanna|J|', 'Sadowska|Joanna|J|', 'Boryczka|Stanisław|S|']
Betulin Betulone Synthesis Cytotoxic activity Lipophilicity