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Molecules 2013, 18(11), 14070-14084; doi:10.3390/molecules181114070

Design, Synthesis and Cytotoxic Activities of Novel Aliphatic Amino-Substituted Flavonoids

1,* , 2
1 College of Life Sciences, China Jiliang University, Hangzhou 310018, Zhejiang, China 2 Hangzhou Hertz Pharmaceutical Co., Ltd., Hangzhou 310018, Zhejiang, China 3 Women's Hospital, School of Medicine, Zhejiang University, Hangzhou 310006, Zhejiang, China
* Authors to whom correspondence should be addressed.
Received: 29 September 2013 / Revised: 31 October 2013 / Accepted: 4 November 2013 / Published: 13 November 2013
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A series of flavonoids 9af, 13b, 13d, 13e and 14af bearing diverse aliphatic amino moieties were designed, synthesized and evaluated for their cytotoxic activities against the ECA-109, A-549, HL-60, and PC-3 cancer cell lines. Most of the compounds exhibited moderate to good activities. The structure-activity relationships were studied, revealing that the chalcone skeleton is the most preferable for cytotoxic activities. Chalcone 9d was the most promising compound due to its high potency against the examined cancer cell lines (its IC50 values against ECA-109, A549, HL-60 and PC-3 cells were 1.0, 1.5, 0.96 and 3.9 μM, respectively).
Keywords: flavonoid; chalcone; synthesis; cytotoxic activity flavonoid; chalcone; synthesis; cytotoxic activity
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Liu, G.; Ge, Z.; Zhao, M.; Zhou, Y. Design, Synthesis and Cytotoxic Activities of Novel Aliphatic Amino-Substituted Flavonoids. Molecules 2013, 18, 14070-14084.

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