Chinese Journal of Organic Chemistry >
Synthesis and Biological Evaluation of 4-Dimethylamino Flavonoid Derivatives
Received date: 2013-09-26
Revised date: 2013-10-29
Online published: 2013-11-05
Supported by
Project supported by the National Natural Science Foundation of China (Nos. 21172053, 21302041), the Postdoctoral Science Foundation of China (No. 2012M521391) and the Postdoctoral Science Foundation of Henan Province (No. BH2011043).
Ten novel 4-dimethylamino flavonoid derivatives were designed and synthesized. The structures of these compounds were confirmed by 1H NMR, ESI-MS and elemental analysis. Their preliminary antitumor activity was evaluated by measuring their cytotoxic activity against the HepG2 cell line using thiazolyl blue tetrazolium bromide (MTT) assay. All ten compounds exhibited potent antitumor activity at 30 mmol/L. Some of the compounds displayed higher activity than the reference compound, quercetin. Compounds 5c, 5e, 5f and 5j were the most potent with inhibition rates of 91.0%, 90.1%, 95.7% and 92.1%, respectively. Moreover, compound 5f at 10 mmol/L showed an inhibition rate of 93.1%. Further investigation is needed.
Key words： flavonoid; derivative; synthesis; antitumor
Su Yabin , Hong Chen , Li Qian , Luo Wen , Wang Chaojie . Synthesis and Biological Evaluation of 4-Dimethylamino Flavonoid Derivatives[J]. Chinese Journal of Organic Chemistry, 2014 , 34(3) : 600 -604 . DOI: 10.6023/cjoc201309034
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