Synthesis and anticancer activity of(+)-nopinone-based 2-amino-3-cyanopyridines  

作　　者：Shengliang LIAO Shibin SHANG Minggui SHEN Xiaoping RAO Hongyan SI Jie SONG Zhanqian SONG 

机构地区：[1]Institute of Chemical Industry of Forest Products,China Academy of Forestry,National Engineering Laboratory for Biomass Chemical Utilization,State Forestry Administration’s Key and Open Laboratory for Forest Chemical Engineering,Jiangsu Provincial Key Laboratory for Biomass Energy and Material,Nanjing 210042,China [2]Department of Chemistry and Biochemistry,University of Michigan-Flint,Flint MI 48502,USA

出　　处：《Frontiers of Agricultural Science and Engineering》2015年第4期335-340,共6页农业科学与工程前沿（英文版）

基　　金：This work was supported by the Joint Funds of the National Natural Science Foundation of China and Yunnan Provincial Government(U1202265).

摘　　要：Twelve(+)-nopinone-based 2-amino-3-cyanopyridines 4a-1 were synthesized from(–)-β-pinene.The structures of these compounds were characterized by FT-IR,1H NMR,and ESI-MS.All the compounds were tested for their anticancer activity against lung cancer cell line A549,gastric cancer cell line MKN45 and breast cancer cell line MCF7 by MTT method,respectively.The results showed that compounds 4f,4j and 4k had promising anticancer activity against these cancer cell lines,in particular,compound 4f exhibited broad-spectrum and highly efficient anticancer activity against cell lines A549,MKN45 and MCF7 with IC50 of 23.78,67.61 and 53.87μmol·L^(-1),respectively.The preliminary analysis of the structure activity relationship implied that the Br or Cl substituted group of the benzene ring in these derivatives significantly contributed to the anticancer activity.

关 键 词：Β-PINENE nopinone SYNTHESIS 2-amino-3-cyanopyridine ANTICANCER 

分 类 号：R73[医药卫生—肿瘤]