Total Synthesis and Cytotoxicity of Tylophorine Analogue DCB-3501
LI Song-tao1, LIU Jiang2, HUANG Xue-shi2
1.Hebei Key Laboratory of Study and Exploitation of Traditional Chinese Medicine, Chengde Medical University, Chengde 067000, China; 2. Institute of Metabolic Disease Research and Drug Development, China Medical University, Shenyang 110122, China
Abstract：The tylophorine analogue DCB-3501 was totally synthesized by a seven-step reaction including Perkin condensation, free radical oxidative coupling, Swern oxidation, reductive amination and Fridel-Crafts acylation, using 3,4-dimethoxy-benzaldehyde and 3,4-dimethoxy-phenylacetic acid as the raw materials. The structure was confirmed by 1H NMR and ESI-MS. The in vitro cytotoxicity results showed that the IC50 of DCB-3501 against human colon cancer cell HCT116, human gastric cancer cell BGC-823, human hepatic cancer cell HepG-2, human cervical cancer cell HeLa and human large-cell lung cancer cell H460 were 20.0 μmol·L-1, 50.9 μmol·L-1, 2.1 μmol·L-1, 65.8 μmol·L-1 and 30.8 μmol·L-1, respectively.
李松涛， 刘江， 黄学石. 娃儿藤碱类似物DCB-3501的全合成及其细胞毒性[J]. 合成化学, 2016, 24(1): 30-34.
LI Song-tao, LIU Jiang, HUANG Xue-shi. Total Synthesis and Cytotoxicity of Tylophorine Analogue DCB-3501. Chinese Journal of Synthetic Chemistry, 2016, 24(1): 30-34.
2016, Vol. 24 
