伏立诺他衍生物N2E的合成、鉴定及体外抗肿瘤活性研究
孙心愿;倪安然;王晓翔;冯冰虹
【期刊名称】《广东药学院学报》 【年(卷),期】2017(033)002
【摘要】Objective To synthesize vorinostat derivative N2E and evaluate its anti-tumor activity.Methods Suberic acid was used as raw material to produce suberoyl anhydride by dehydration in the presence of acetic anhydride,then acetic anhydride ring opening and amidation with 2-ethoxy aniline in dichloromethane at 0 ℃,and eventually N2E was produced by esterification and aminolysis.The structure of N2E was identified by MS,1H NMR and 13C NMR.The inhibitory activity of N2E against lung cancer NCI-H1299,NCI-H460,A549 cells and glioma U251,MGR2 cell lines were investigated and the cytotoxicity to LO-2 cells was observed.Results The target compound was identified as vorinostat
derivative
the
N2E purity
[N-(2-ethoxyphenyl)-N′-was
about
99.1%
by
hydroxyoctanediamide],and
normalization method.The inhibitory effect of N2E on human lung cancer cells NCI-H1299,A549 and glioma cells U251,MGR2 were stronger than that of vorinostat (P<0.001),however the cytotoxicity of N2E on human normal liver cells LO-2 was weaker than that of vorinostat (P<0.001).Conclusion N2E was successfully synthesized by mixed anhydride method,and the inhibitory effect on NCI-
伏立诺他衍生物N2E的合成、鉴定及体外抗肿瘤活性研究
