(1~iR,1^(ii)R,2~iR,2^(ii)R)-N^i,N^(ii)-(1,3-亚苯基双(亚甲基))环己烷-1,2-二胺作为配体的双核铂配合物的合成及其抗癌活性  

Synthesis and Antitumor Activity of Dinuclear Platinum Complexes with (1~iR, 1^(ii)R, 2~iR, 2^(ii)R)-N^i, N^(ii)-(1, 3-Phenylenebis(methylene))dicyclohexane-1, 2-diamie as the Ligand

作　　者：高传柱[1,2] 陈骥[1] 王天帅[1] 张艳[1] 钱韵旭[1] 杨波[1] 苟少华[3] 董鹏[2] 张英杰[2] 

机构地区：[1]昆明理工大学生命科学与技术学院,昆明650500 [2]昆明理工大学材料科学与工程学院,昆明650504 [3]东南大学化学与化工学院药物研究中心,南京211189

出　　处：《无机化学学报》2015年第11期2188-2196,共9页Chinese Journal of Inorganic Chemistry

基　　金：国家自然科学基金(No.21361014;21302074);国家自然科学基金(No.21362016);教育部博士点基金(No.20125314120007)资助项目

摘　　要：以(1iR,1iiR,2iR,2iiR)-Ni,Nii-(1,3-亚苯基双(亚甲基))环己烷-1,2-二胺(HL)作为配体,设计并合成了7种双核铂配合物,并利用IR,1H NMR,13C NMR,ESI-MS和元素分析等进行了表征。通过MTT法测定目标双核铂配合物对人类Hep G-2,A549,HCT-116和MCF-7四种癌细胞系的细胞毒性。结果表明,所有的化合物对Hep G-2,A549和HCT-116细胞系均表现了良好的细胞毒活性,但对MCF-7细胞系均无活性。其中,以3-羟基环丁烷-1,1-二羧酸为离去基团的配合物P7对HepG-2和A549细胞系的活性优于卡铂,对HCT-116细胞系的活性接近于奥沙利铂。Seven diculear platinum complexes with the new chiral ligand, （1iR,1iiR,2iR,2iiR）-Ni,Nii-（1,3- phenylenebis（methylene））dieyclohexane-1,2-diamine （HL）, were designed, synthesized and speetrally characterized by IR, 1H NMR, 13C NMR, ESI-MS and microanalyses. The cytotoxicities of targeted dinuclear platinum compounds against human HepG-2, A549, HCT-116 and MCF-7 cell lines were evaluated by MTT assay. Results indicated that all compounds exhibited positive activity to HepG-2, A549 and HCT-116 cell lines, but none of them showed activity to MCF-7 cell line. Among them, compound PT, owing to 3-hydroxycyclobutane-1,1- diearboxylate as the leaving group, gave better antitumor activity than carboplatin against HepG-2 and A549 cell lines, and close eytotoxicity to oxaliplatin against HCT-116 cell line.

关 键 词：双核铂(Ⅱ)配合物 手性配体 体外细胞毒性 

分 类 号：O614.82[理学—无机化学]