顺式-草酸-二霉酚酸-(反式-1,2-环己烷二胺)合铂(Ⅳ)的合成、表征及抗肿瘤活性  

Synthesis,Characterization and Anticancer Activity of Cis-oxalate-dimycophenolic Acid-(trans-1,2-cyclohexanediamine)platinum(Ⅳ)

作　　者：刘其星 王应飞 谢丽娇 丛艳伟 曾艳 孙明能 沈庆飞 LIU Qixing;WANG Yingfei;XIE Lijiao;CONG Yanwei;ZENG Yan;SUN Mingneng;SHEN Qingfei(Kunming Guiyan Pharmaceutical Co.,Ltd.,Kunming 650106,China;College of Vocational and Technical Education,Yunnan Normal University,Kunming 650500,China)

机构地区：[1]昆明贵研药业有限公司,云南昆明650106 [2]云南师范大学职业技术教育学院,云南昆明650500

出　　处：《合成化学》2023年第1期61-66,共6页Chinese Journal of Synthetic Chemistry

基　　金：昆明贵研药业有限公司科技创新基地建设项目(202107AB110003)。

摘　　要：设计并合成了一种新型铂(Ⅳ)配合物:顺式-草酸-二霉酚酸-(反式-1,2-环己烷二胺)合铂(Ⅳ),采用元素分析、质谱、红外光谱和核磁共振表征了配合物的组成和化学结构,并采用溴化噻唑蓝四氮唑(MTT)比色法对目标化合物进行抗肿瘤活性评价。结果表明:配合物结构与预期设想一致,并对4种常见癌细胞(SW480、HCT-116、A2780和U-2OS)有明显抑制活性,以给药最高浓度计,抑制率分别为37.43%、71.56%、33.27%和65.23%。A new platinum(Ⅳ)complex,cis-oxalate-dimycophenolic acid-(trans-1,2-cyclohexanediamine)platinum(Ⅳ),was designed and synthesized.The structure was characterized by elemental analysis(EA),mass spectrometry(MS),Fourier transform infrared spectrometry(FT-IR)and nuclear magnetic resonance(NMR).The antitumor activity of the target compound was evaluated by methyl thiazolyl(MTT)method.The results showed that the structure of the compound was consistent with the expected assumption,and it had obvious inhibitory activity on the growth of 4 common cancer cells(SW480,HCT-116,A2780 and U-2OS).With the highest concentration of administration,the inhibition rates were 37.43%,71.56%,33.27%and 65.23%respectively.

关 键 词：铂(Ⅳ)配合物 合成 表征 抗肿瘤活性 顺反结构 草酸 

分 类 号：O627.8[理学—有机化学]