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

Author(s): Songtao Li*, Hongling Zhao, Zhifeng Yin, Shuhua Deng, Yang Gao, Yunfeng Li, Tao Dai.

Journal Name: Letters in Organic Chemistry

Volume 16 , Issue 6 , 2019

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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.

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Article Details

VOLUME: 16
ISSUE: 6
Year: 2019
Page: [462 - 467]
Pages: 6
DOI: 10.2174/1570178615666181025115513
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