Synthesis and cytotoxicity of 3-arylacrylic ester derivatives of the simplified saframycin-ecteinascidin skeleton prepared from L-dopa

DONG Wenfang; GUO Ju; LIU Wei; YAN Zheng; WANG Nan; LIU Zhanzhu

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Synthesis and cytotoxicity of 3-arylacrylic ester derivatives of the simplified saframycin-ecteinascidin skeleton prepared from L-dopa

DONG Wenfang,GUO Ju,LIU Wei,YAN Zheng,WANG Nan,LIU Zhanzhu * #

State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing, 100050

*Correspondence author

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Funding: Specialized Research Fund for the Doctoral Program of Higher Education （No.No. 200800230030, No. 20101106110030）

Opened online:15 March 2013

Accepted by: none

Citation: DONG Wenfang,GUO Ju,LIU Wei.Synthesis and cytotoxicity of 3-arylacrylic ester derivatives of the simplified saframycin-ecteinascidin skeleton prepared from L-dopa[OL]. [15 March 2013] http://en.paper.edu.cn/en_releasepaper/content/4527983

Fifteen simplified tetrahydroisoquinoline analogues were prepared from L-dopa. The in vitro antitumor activities of these analogues were evaluated against HCT-8, BEL-7402, BGC-823, A549, A2780, MCF-7 and MX-1 cell lines. The IC50 values of the cytotoxicity of most analogues were at the level of 10-7M or 10-8M. Compound 17 with 2,3,4-trimethoxycinnamate side chain at C-22 showed the most potent antitumor activity.

Keywords:Synthesis; Antitumor activity; Tetrahydroisoquinoline; L-dopa;

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