新型白杨素类 1,2,3-三唑衍生物的合成及抗癌活性评价。
Synthesis and Biological Evaluation of New 1,2,3-Triazole Derivatives of the Chrysin Flavonoid as Anticancer Agents.
机构信息
Department of Chemistry, Osmania University, Hyderabad - 500007, Telangana, India.
Chemical Engineering, Arizona State University, Tempe, AZ 85287-6106, USA.
出版信息
Anticancer Agents Med Chem. 2022;22(1):160-168. doi: 10.2174/1871520621666210315090527.
BACKGROUND AND OBJECTIVE
Chrysin and its derivatives proved to possess potential anti-tumour activity.
MATERIALS AND METHODS
A new series of chrysin analogs containing 1,2,3-triazoles with different substituent groups (5a-5l) was designed, synthesized, and evaluated as potential anticancer agents. The synthesized compounds were characterized using FT-IR, 1H NMR 13C NMR spectroscopy and mass spectrometry.
RESULTS
The anticancer activities of the synthesized compounds were studied in four cancer cell lines viz. PC3, PC3-PSMA, MCF-7 and UM-UC-3 using doxorubicin as standard. Among all the tested compounds, 5c was found as most active with IC50 value of 10.8 ± 0.04 μM in PC3 cells and 20.53 ± 0.21 μMin MCF-7 cells, respectively. Flow cytometry analyses indicated that synthesized compounds 5a, 5c, and 5h arrested MCF-7 cells at the G2/M phase in a dose-dependent manner.
CONCLUSION
Chyrsin derivatives could be novel anticancer agents.
背景与目的
白杨素及其衍生物被证明具有潜在的抗肿瘤活性。
材料与方法
设计、合成了一系列含有不同取代基的 1,2,3-三唑的白杨素类似物（5a-5l），并将其评估为潜在的抗癌药物。合成的化合物通过傅里叶变换红外光谱（FT-IR）、1H NMR 13C NMR 光谱和质谱进行了表征。
结果
用阿霉素作为标准，在四种癌细胞系（PC3、PC3-PSMA、MCF-7 和 UM-UC-3）中研究了合成化合物的抗癌活性。在所测试的所有化合物中，化合物 5c 在 PC3 细胞中的 IC50 值为 10.8±0.04 μM，在 MCF-7 细胞中的 IC50 值为 20.53±0.21 μM，表现出最强的活性。流式细胞术分析表明，合成化合物 5a、5c 和 5h 以剂量依赖的方式将 MCF-7 细胞阻滞在 G2/M 期。
结论
白杨素衍生物可能是新型的抗癌药物。
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