Wei Can-Jing, Xu Fang, Shi Meng-Jiao, Hu Jia-Wen, Wang Jia-Jia, Zhen Bo, Wang Xue, Ji Teng-Fei, Wang Jin-Hua, Du Guan-Hua
a State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica , Chinese Academy of Medical Sciences and Peking Union Medical College , Beijing 100050 , China.
b Beijing Key Laboratory of Drug Targets Identification and Drug Screening, Institute of Materia Medica , Chinese Academy of Medical Sciences and Peking Union Medical College , Beijing 100050 , China.
J Asian Nat Prod Res. 2018 Mar;20(3):277-291. doi: 10.1080/10286020.2017.1386659. Epub 2017 Nov 1.
A series of new sinomenine derivatives were designed, synthesized, and evaluated in tumor inhibitory activity, such as human triple negative breast cancer cell line (MDA-MB-231), glioma cell line (A172), human lung cancer cell line (A549), human colon cancer cell line (HCT-8). The modifications were carried out on rings A and C of the sinomenine by esterificating on phenolic hydroxyl with good yields. The highlight of this work was that the synthetic procedures were concise and sinomenine derivatives demonstrated promising antitumor activities.
设计、合成了一系列新的青藤碱衍生物，并对其在肿瘤抑制活性方面进行了评估，如人三阴性乳腺癌细胞系（MDA-MB-231）、胶质瘤细胞系（A172）、人肺癌细胞系（A549）、人结肠癌细胞系（HCT-8）。通过对青藤碱的A环和C环上的酚羟基进行酯化修饰，获得了较高的产率。这项工作的亮点在于合成步骤简洁，且青藤碱衍生物显示出有前景的抗肿瘤活性。
