Abstract
23-Hydroxybetulinic acid (1) served as the precursor for the synthesis of C-28 ester derivatives. The target compounds were evaluated in vitro for their antitumor activities against five cell lines (A549, BEL-7402, SF-763, B16 and HL-60). Among the obtained compounds, 6i had the most potent antitumor activity, with the IC(50 values of 8.35 µM in HL-60 cells and showed similar antitumor activity as cyclophosphamide in H22 liver tumor and as 5-fluorouracil in B16 melanoma in vivo.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacology
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Cell Line, Tumor
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Cell Survival / drug effects
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Cyclophosphamide / pharmacology
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Esters
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Female
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Fluorouracil / pharmacology
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Humans
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Inhibitory Concentration 50
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Mice
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Mice, Inbred ICR
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Triterpenes / chemical synthesis*
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Triterpenes / pharmacology
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Tumor Burden / drug effects
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Xenograft Model Antitumor Assays
Substances
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23-hydroxybetulinic acid
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Antineoplastic Agents
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Esters
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Triterpenes
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Cyclophosphamide
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Fluorouracil