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Citation: ZHAO Jina, XIE Huan-Xub, LIU Hong-Yub, MA HongXiab, XIE Song-Qiangc, WANG Chao-Jie. Synthesis and Cytotoxicity of N,N-Bis(8-flavonmethyl) geranylamine Derivatives[J]. Chinese Journal of Applied Chemistry, ;2010, 27(4): 398-403. doi: 10.3724/SP.J.1095.2010.90334 shu

Synthesis and Cytotoxicity of N,N-Bis(8-flavonmethyl) geranylamine Derivatives

a. Key Laboratory of Natural Medicine and Immune Engineering, Henan University, Kaifeng 475004;
b. College of Chemistry and Chemical Engineering, Henan University, Kaifeng 475004;
c. College of Pharmacy, Henan University, Kaifeng 475004

Received Date: 8 May 2009
Revised Date: 29 July 2009

Four N,N-bis(8-flavonmethyl)geranylamine derivatives were designed and synthesized.The structures of the synthesized compounds were determined from the results of ¹H NMR,MS and elemental analysis.The prelimilary cytotoxicity was evaluated on K562 and SMMC₇721 cell lines by MTT assay.The results demonstrate that all the compounds possess antitumor actitity and compound 1c is the best among them with an IC₅₀ value of 5.78 μmol/L or 3.85 μmol/L against K562 or SMMC₇721 cell lines,respectively.The in vitro antitumor activities of compounds 1a and 1c against K562 were better than that of the commercial drug Melphalan.The interaction of compound 1c with herring sperm DNA was explored with ethidium bromide(EB) as a fluorescence probe.The result of the study on fluorescence quenching by DNA-EB confirms the strong interaction of compound 1c with Herring Sperm DNA.
- N,N-bis(flavonmethyl)geranylamine,
- synthesis,
- cytotoxicity,
- fluorescence probe
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