Synthesis and cytotoxicity of triterpenoids derived from betulin and betulinic acid via click chemistry |
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Authors: | Wei Shi Ning Tang |
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Institution: | Department of Chemistry, Zhejiang University, Hangzhou310027, China |
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Abstract: | 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 μM) against leukemia cell-line HL-60 (eight- to ninefold higher potency than betulinic acid). |
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Keywords: | betulin betulinic acid derivatives click chemistry cytotoxicity |
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