双醋瑞因氨基膦酸酯类衍生物的合成及抗肿瘤活性研究
The Synthesis and Antitumor Activity Evaluation of Diacerein Amino Phosphonate Derivatives

以大黄酸、氨基膦酸酯为原料,合成4个新型乙酰化大黄酸的α-氨基膦酸酯类衍生物,并利用IR、1H NMR、13C NMR、31P NMR、ESI-MS和元素分析对化合物的结构进行表征.用MTT方法评价它们在体外对人肝癌(HepG-2)、人鼻咽癌(CNE)、人肺腺癌细胞(Spca-2)和人肺腺癌细胞(Hct-116)株的生长抑制活性.新合成的化合物均具有潜在的体外抑制癌细胞生长活性,尤其是化合物4d表现出了最强的抑制活性,且对人正常的脐静脉内皮细胞具有低毒性.
The diacerein amino phosphonate derivatives were synthesized starting from rhein and amino phosphonate to obtain four target compounds.The structures of compopnds were confirmed by IR、H NMR、C NMR 、P NMR、ESI-MS spectra and elementary analyses,and their invitro anticancer activity against the four cancer celllines of HepG-2、CNE、Spca-2、Hct-116 was evlauate by MTT,four compounds were synthesized with the potential inhibitory growth of cancer cells in vitro,especially the compound of 4d showed the significant inhibitory activity,and for HUVEC cell with low toxicity