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

Molecules

Guannan Liu²  Zhen Ge¹  Mengdan Zhao³ 

[1] Hangzhou Hertz Pharmaceutical Co., Ltd., Hangzhou 310018, Zhejiang, China; E-Mail:;College of Life Sciences, China Jiliang University, Hangzhou 310018, Zhejiang, China;Women’s Hospital, School of Medicine, Zhejiang University, Hangzhou 310006, Zhejiang, China; E-Mail:

关键词: flavonoid;    chalcone;    synthesis;    cytotoxic activity;   

DOI  :  10.3390/molecules181114070

来源: mdpi

【 摘 要 】

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).

【 授权许可】

CC BY   
© 2013 by the authors; licensee MDPI, Basel, Switzerland.