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Citation: ZHAO Jin, ZHAO Yong-Mei, LUO Wen, XIE Song-Qiang, WANG Chao-Jie. Synthesis and Biological Antitumor of New Aryl Nitrogen Mustards[J]. Chinese Journal of Applied Chemistry, ;2008, 25(1): 38-42. shu

Synthesis and Biological Antitumor of New Aryl Nitrogen Mustards

1.
College of Chemistry and Chemical Engineering, Henan University, Kaifeng 475001

Corresponding author: WANG Chao-Jie,
Received Date: 14 January 2007
Available Online: 30 May 2007
Fund Project: 河南省科技攻关项目(496410030) (496410030)

Six aryl nitrogen mustard derivatives were designed and synthesized with N,N-di(2-chloroethyl)-1,4-phenylene diamine(4) as the pharmacophore,terpineols and linear saturated alcohols as the carrier,and carbamate as the linker.The yields for the target compounds were between 66%~90%.The structures of the compounds were confirmed by ¹H NMR,¹³C NMR,MS and elemental analysis.The in vitro anti-tumor activities of these compounds were tested preliminarily on B16,K562,and CHO cells.The results demonstrate that some compounds possessed higher activity than reference compound 4,and were similar to the commercial drug Melphalan in certain range of concentrations.The in vitro inhibition of farnesyl modified compound 6e against B16 was even better than that of Melphalan at a concentration of 0.1~10 μmol/L.
- aryl nitrogen mustard,
- alcohol,
- synthesis,
- biological activity
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