Journal
JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH
Volume 17, Issue 2, Pages 159-169Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/10286020.2014.979164
Keywords
betulin; betulinic acid; cytotoxicity; derivatives; click chemistry
Funding
- National Natural Science Foundation of China [81173640]
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In this study, a series of triazole substituted betulin and betulinic acid derivatives was designed and synthesized via click chemistry at C-30 position. Eighteen target compounds were evaluated in vitro for their antitumor activities against leukemia cell-line HL-60. Seventeen compounds have not reported before. The cytotoxic experiment showed that most of betulinic acid derived triazoles have higher cytotoxic profile than betulinic acid. Among them, compound 30-[4-(4-fluorophenyl)-1H-1,2,3-triazol-1-yl] betulinic acid (7b) showed the best IC50 value (1.3 mu M) against leukemia cell-line HL-60 (eight- to ninefold higher potency than betulinic acid).
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