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| 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 |
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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.
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Received: 27 July 2015
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2016, Vol. 24 
