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CHEMISTRY OF NATURAL COMPOUNDS · 2025 · IF 0.9

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

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

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 IC 50 value for the inhibitory activity of compound 5e against human breast cancer cells (MCF-7) was 11.2 μmol/L.

研究领域: 药物化学 · 有机合成 · 肿瘤药理学 · 天然产物衍生物

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CHEMISTRY OF NATURAL COMPOUNDS · 2024 ·Vol. 60 ·期 1 ·92-97 · IF 0.8

Synthesis of Novel Stigmasterol Derivatives with 1,2,3-Triazole Substituent at the C-3 Position and Their Cytotoxicity Toward HeLa, HGC-27, and HEK-293T Cells

Wang Yong,Wang Wei,Liu Cong-Jun,Gao Song,Xiong Yong-Ge,Gao Tian-Zeng,Li Wei-Shi,Li Jing-Jing

Eight new stigmasterol derivatives possessing 1,2,3-triazoles moiety were synthesized by a 1,3-dipolar cycloaddition reaction. All the compounds were characterized by IR, NMR, and HR-MS. In addition, human cervical cancer cells (HeLa), human gastric cancer cells (HGC-27), and human renal epithelial cells (HEK-293T) were selected to study the antitumor activity of the synthesized compounds. The results demonstrated that compounds 3c and 3d exhibited better inhibitory activity against the tested tumor cell lines. The IC 50 value of the inhibitory activity on HeLa was 52.3 μmol·L –1 and 31.4 μmol·L –1 , and 40.6 μmol·L –1 and 44.6 μmol·L –1 for HGC-27, respectively.

研究领域: 有机合成 · 药物化学 · 药理学 · 癌症研究 · 细胞生物学

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

Synthesis of Novel Stigmasterol Derivatives with 1,2,3-Triazole Substituent at the C-3 Position and Their Cytotoxicity Toward HeLa, HGC-27, and HEK-293T Cells