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Design, Synthesis and Cytotoxic Activities of Novel Aliphatic Amino-Substituted Flavonoids
College of Life Sciences, China Jiliang University, Hangzhou 310018, Zhejiang, China
Hangzhou Hertz Pharmaceutical Co., Ltd., Hangzhou 310018, Zhejiang, China
Women's Hospital, School of Medicine, Zhejiang University, Hangzhou 310006, Zhejiang, China
* Authors to whom correspondence should be addressed.
Received: 29 September 2013; in revised form: 31 October 2013 / Accepted: 4 November 2013 / Published: 13 November 2013
Abstract: A series of flavonoids 9a–f, 13b, 13d, 13e and 14a–f 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
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MDPI and ACS Style
Liu, G.; Ge, Z.; Zhao, M.; Zhou, Y. Design, Synthesis and Cytotoxic Activities of Novel Aliphatic Amino-Substituted Flavonoids. Molecules 2013, 18, 14070-14084.
Liu G, Ge Z, Zhao M, Zhou Y. Design, Synthesis and Cytotoxic Activities of Novel Aliphatic Amino-Substituted Flavonoids. Molecules. 2013; 18(11):14070-14084.
Liu, Guannan; Ge, Zhen; Zhao, Mengdan; Zhou, Yifeng. 2013. "Design, Synthesis and Cytotoxic Activities of Novel Aliphatic Amino-Substituted Flavonoids." Molecules 18, no. 11: 14070-14084.