<p>A series of abietic acid derivatives modified with a triazole moiety at the C-18 position were synthesized using Huisgen 1,3-dipolar cycloaddition reaction of 18-azidoabietane with alkynes. The antitumor activity of the synthesized compounds was investigated through human cervical cancer cells (HeLa), human breast cancer cells (MCF-7) and human renal epithelial cells (HEK-293T). The outcome indicated that compounds <b>5e</b>, <b>5f</b>, <b>5j</b> exhibited positive inhibitory activity against the tested tumor cell lines. In particular, the IC<sub>50</sub> value for the inhibitory activity of compound <b>5e</b> against human breast cancer cells (MCF-7) was 11.2 μmol/L.</p>

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Synthesis and Cytotoxicity of New 1,2,3-Triazole Derivatives of Abietic Acid

  • Yong Wang,
  • Wei Wang,
  • Li-Na Liu,
  • Dong-Lin Wei,
  • Cong-Jun Liu,
  • Shang-Hua Wei,
  • Song Gao,
  • Shu-Ping Yu,
  • Ning Yao,
  • Yu-Fei Wang

摘要

A series of abietic acid derivatives modified with a triazole moiety at the C-18 position were synthesized using Huisgen 1,3-dipolar cycloaddition reaction of 18-azidoabietane with alkynes. The antitumor activity of the synthesized compounds was investigated through human cervical cancer cells (HeLa), human breast cancer cells (MCF-7) and human renal epithelial cells (HEK-293T). The outcome indicated that compounds 5e, 5f, 5j exhibited positive inhibitory activity against the tested tumor cell lines. In particular, the IC50 value for the inhibitory activity of compound 5e against human breast cancer cells (MCF-7) was 11.2 μmol/L.