Molecules 2010, 15(11), 7871-7883; doi:10.3390/molecules15117871
Article

Synthesis and Tumor Cytotoxicity of Novel Amide Derivatives of β-Hederin

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Received: 9 October 2010; in revised form: 1 November 2010 / Accepted: 2 November 2010 / Published: 3 November 2010
(This article belongs to the Special Issue Phenolics and Polyphenolics)
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Abstract: Thirteen novel triterpenoid saponins, designed as amide derivatives of the natural cytotoxic saponin β-hederin, were synthesized by a stepwise glycosylation strategy. The in vitro cytotoxic activity of these compounds was evaluated against five different tumor cell lines. Most of the evaluated compounds showed effective inhibitory activity against at least one tumor cell line at micromolar concentrations. The preliminary structure-activity relationships (SAR) indicate that mide derivatization at C-28 resulted in highly cytotoxic derivatives on specific tumor cell lines, and also resulted in an increase in the antitumor selectivity of β-hederin. 
Keywords: triterpenoid saponins; β-hederin; tumor cytotoxicity; synthesis
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MDPI and ACS Style

Liu, Y.; Lu, W.-X.; Yan, M.-C.; Yu, Y.; Ikejima, T.; Cheng, M.-S. Synthesis and Tumor Cytotoxicity of Novel Amide Derivatives of β-Hederin. Molecules 2010, 15, 7871-7883.

AMA Style

Liu Y, Lu W-X, Yan M-C, Yu Y, Ikejima T, Cheng M-S. Synthesis and Tumor Cytotoxicity of Novel Amide Derivatives of β-Hederin. Molecules. 2010; 15(11):7871-7883.

Chicago/Turabian Style

Liu, Yang; Lu, Wen-Xiang; Yan, Mao-Cai; Yu, Yang; Ikejima, Takashi; Cheng, Mao-Sheng. 2010. "Synthesis and Tumor Cytotoxicity of Novel Amide Derivatives of β-Hederin." Molecules 15, no. 11: 7871-7883.


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