通过-氨化合成黄酮衍生物及其抗癌活性评价。
Synthesis of Flavone Derivatives via -Amination and Evaluation of Their Anticancer Activities.
机构信息
State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang 550014, China.
The Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences/Guizhou Provincal Engineering Research Center for Natural Drugs, Guiyang 550014, China.
出版信息
Molecules. 2019 Jul 26;24(15):2723. doi: 10.3390/molecules24152723.
Seventeen new flavone derivatives substituted at the 4'-OH position were designed, synthesized and evaluated for their anticancer and antibacterial activities. Among them, compounds , , , , , and demonstrated the most potent antiproliferative activities against a human erythroleukemia cell line (HEL) and a prostate cancer cell line (PC3). The results also showed that the IC value of compounds , , , , , and were close to that of the anticancer drug cisplatin (DDP) and lower than that of apigenin. All of the derivatives did not present antibacterial activities. The structure-activity relationships evaluation showed that the configuration of methyl amino acid might affect their biological activities.
设计、合成了 17 种在 4'-OH 位取代的黄酮衍生物，并评价了它们的抗癌和抗菌活性。其中，化合物 、 、 、 、 、 和 对人红白血病细胞系（HEL）和前列腺癌细胞系（PC3）表现出最强的增殖抑制活性。结果还表明，化合物 、 、 、 、 、 的 IC 值接近抗癌药物顺铂（DDP），低于芹菜素。所有的衍生物都没有表现出抗菌活性。构效关系评价表明，甲基氨基酸的构型可能影响它们的生物活性。
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