Synthesis and biological evaluation of bufalin-3-yl nitrogen-containing-carbamate derivatives as anticancer agents

• Highly efficient method to synthesize bufalin-3-yl nitrogen-containing-carbamate derivatives.
• Bufalin-3-yl nitrogen-containing-carbamate derivatives show significant cytotoxicity.
• 3i-HCl significantly inhibits tumor growth in vivo by 100% at the dose 2 mg/kg by iv, or 4 mg/kg by ig.

A series of bufalin-3-yl nitrogen-containing-carbamate derivatives 3 were designed, synthesized, and evaluated for their proliferation inhibition activities against human cervical epithelial adenocarcinoma (HeLa) cell line. The structure–activity relationships (SARs) of this new series are described in this paper. Cytotoxicity data revealed that the C3 moiety had an important influence on cytotoxic activity. Compound 3i-HCl exhibited significant in vitro antiproliferative activity against the ten tested tumor cell lines, with IC50 values ranging from 0.30 to 1.09 nM. Furthermore, 3i-HCl can significantly inhibit tumor growth by 100% at the dose 2 mg/kg by iv, or 4 mg/kg by ig.

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