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Synthesis and Antitumor Activity Evaluation of New Phenanthrene-Based Tylophorine Derivatives

[ Vol. 16 , Issue. 6 ]

Author(s):

Songtao Li*, Hongling Zhao, Zhifeng Yin, Shuhua Deng, Yang Gao, Yunfeng Li and Tao Dai   Pages 462 - 467 ( 6 )

Abstract:


A series of new phenanthrene-based tylophorine derivatives (PBTs) were synthesized in good yield and their structures were characterized by 1H-NMR spectroscopy and ESI MS. In vitro antitumor activity of these compounds against five human carcinoma cell lines, including HCT116 (colorectal), BGC-823 (gastric), HepG-2 (hepatic), Hela (cervical) and H460 (lung) cells, was evaluated by MTT assay. Among these PBTs, compound 6b showed the highest antitumor activities against HCT116 and HepG-2 cell lines with IC50 values of 6.1 and 6.4 μM, respectively, which were comparable to that of adriamycin hydrochloride. The structure-activity relationship of these compounds was also discussed based on the results of their antitumor activity.

Keywords:

Synthesis, phenanthrene, tylophorine, derivative, antitumor, cytotoxicity.

Affiliation:

Hebei Province Key Laboratory of Research and Development of Traditional Chinese Medicine, Institute of Traditional Chinese Medicine, Chengde Medical University, Chengde, Hebei 067000, Hebei Province Key Laboratory of Research and Development of Traditional Chinese Medicine, Institute of Traditional Chinese Medicine, Chengde Medical University, Chengde, Hebei 067000, Hebei Province Key Laboratory of Research and Development of Traditional Chinese Medicine, Institute of Traditional Chinese Medicine, Chengde Medical University, Chengde, Hebei 067000, Hebei Province Key Laboratory of Research and Development of Traditional Chinese Medicine, Institute of Traditional Chinese Medicine, Chengde Medical University, Chengde, Hebei 067000, Hebei Province Key Laboratory of Research and Development of Traditional Chinese Medicine, Institute of Traditional Chinese Medicine, Chengde Medical University, Chengde, Hebei 067000, Hebei Province Key Laboratory of Research and Development of Traditional Chinese Medicine, Institute of Traditional Chinese Medicine, Chengde Medical University, Chengde, Hebei 067000, Hebei Province Key Laboratory of Research and Development of Traditional Chinese Medicine, Institute of Traditional Chinese Medicine, Chengde Medical University, Chengde, Hebei 067000



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