Journal
MEDICINAL CHEMISTRY RESEARCH
Volume 26, Issue 1, Pages 1-8Publisher
SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-016-1713-9
Keywords
Betulin; Betulone; Synthesis; Cytotoxic activity; Lipophilicity
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Funding
- Medical University of Silesia in Katowice, Poland [KNW-1-002/N/5/0]
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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 A mu g/mL.
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