Chemistry of Natural Compounds ( IF 0.8 ) Pub Date : 2024-01-30 , DOI: 10.1007/s10600-024-04261-2 Yong Wang , Wei Wang , Cong-Jun Liu , Song Gao , Yong-Ge Xiong , Tian-Zeng Gao , Wei-Shi Li , Jing-Jing Li
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 IC50 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.
中文翻译:
C-3 位带有 1,2,3-三唑取代基的新型豆甾醇衍生物的合成及其对 HeLa、HGC-27 和 HEK-293T 细胞的细胞毒性
通过1,3-偶极环加成反应合成了八种具有1,2,3-三唑部分的新豆甾醇衍生物。所有化合物均通过 IR、NMR 和 HR-MS 进行了表征。此外,还选择人宫颈癌细胞(HeLa)、人胃癌细胞(HGC-27)和人肾上皮细胞(HEK-293T)来研究合成化合物的抗肿瘤活性。结果表明,化合物3c和3d对测试的肿瘤细胞系表现出更好的抑制活性。对HeLa的抑制活性的IC 50值分别为52.3 μmol·L –1和31.4 μmol·L –1,对HGC-27 的抑制活性为40.6 μmol·L –1和44.6 μmol·L –1。