A total of 16 targeted NO-releasing betulinic acid (BA) derivatives were designed and synthesized as
potential anticancer agents. Most IC50 values were under 1.0 μM in vitro test against HepG2 and B16. The result
suggested that derivatives of BA with α,β-unsaturated ketone skeleton possessed significant cytotoxic activities than
the others, among which derivatives with three carbons in diol linker (15b and 15c) exhibited the highest anti-cancer
activity. NO-releasing amount detection of partial target compounds suggested that NO-releasing amount of this series
of BA derivatives positively correlates with their cytotoxic activities. The anti-angiogenic activity of partial target
compounds on zebrafish embryos in our experiment did not show any effects on the SIVs, however, they exhibited
different influence on ISVs, with only 15a and 15d better than the negative control.
Keywords: Betulinic acid derivatives, cytotoxic activities, NO-releasing, anti-angiogenic activity.
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