| (1iR, 1iiR, 2iR, 2iiR)-Ni, Nii-(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 |
| |
| 引用本文： | 高传柱,陈骥,王天帅,张艳,钱韵旭,杨波,苟少华,董鹏,张英杰.(1iR, 1iiR, 2iR, 2iiR)-Ni, Nii-(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[J].无机化学学报,2015,31(11):2188-2196. |
| |
| 作者姓名： | 高传柱 陈骥 王天帅 张艳 钱韵旭 杨波 苟少华 董鹏 张英杰 |
| |
| 作者单位： | 昆明理工大学生命科学与技术学院, 昆明 650500;昆明理工大学材料科学与工程学院, 昆明 650504,昆明理工大学生命科学与技术学院, 昆明 650500,昆明理工大学生命科学与技术学院, 昆明 650500,昆明理工大学生命科学与技术学院, 昆明 650500,昆明理工大学生命科学与技术学院, 昆明 650500,昆明理工大学生命科学与技术学院, 昆明 650500,东南大学化学与化工学院药物研究中心, 南京 211189,昆明理工大学材料科学与工程学院, 昆明 650504,昆明理工大学材料科学与工程学院, 昆明 650504 |
| |
| 基金项目： | 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HepG-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HepG-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。
|
| 关 键 词： | 双核铂(Ⅱ)配合物 手性配体 体外细胞毒性 |
| 收稿时间： | 2015/6/10 0:00:00 |
| 修稿时间： | 2015/8/23 0:00:00 |
Synthesis and Antitumor Activity of Dinuclear Platinum Complexes with (1iR, 1iiR, 2iR, 2iiR)-Ni, Nii-(1, 3-Phenylenebis(methylene))dicyclohexane-1, 2-diamie as the Ligan |
| |
| GAO Chuan-Zhu,CHEN Ji,WANG Tian-Shuai,ZHANG Yan,QIAN Yun-Xu,YANG Bo,GOU Shao-Hu,DONG Peng and ZHANG Ying-Jie.Synthesis and Antitumor Activity of Dinuclear Platinum Complexes with (1iR, 1iiR, 2iR, 2iiR)-Ni, Nii-(1, 3-Phenylenebis(methylene))dicyclohexane-1, 2-diamie as the Ligan[J].Chinese Journal of Inorganic Chemistry,2015,31(11):2188-2196. |
| |
| Authors: | GAO Chuan-Zhu CHEN Ji WANG Tian-Shuai ZHANG Yan QIAN Yun-Xu YANG Bo GOU Shao-Hu DONG Peng and ZHANG Ying-Jie |
| |
| Institution: | Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming 650500, China;Faculty of Materials Science and Engineering, Kunming University of Science and Technology, Kunming 650504, China,Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming 650500, China,Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming 650500, China,Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming 650500, China,Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming 650500, China,Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming 650500, China,Pharmaceutical Research Center, School of Chemistry and Chemical Engineering, Southeast University, Nanjing 211189, China,Faculty of Materials Science and Engineering, Kunming University of Science and Technology, Kunming 650504, China and Faculty of Materials Science and Engineering, Kunming University of Science and Technology, Kunming 650504, China |
| |
| Abstract: | Seven diculear platinum complexes with the new chiral ligand, (1iR,1iiR,2iR,2iiR)-Ni, Nii-(1,3-phenylenebis(methylene))dicyclohexane-1,2-diamine (HL), were designed, synthesized and spectrally 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 P7, owing to 3-hydroxycyclobutane-1,1-dicarboxylate as the leaving group, gave better antitumor activity than carboplatin against HepG-2 and A549 cell lines, and close cytotoxicity to oxaliplatin against HCT-116 cell line. |
| |
| Keywords: | |
|
| 点击此处可从《无机化学学报》浏览原始摘要信息 |
| 点击此处可从《无机化学学报》下载免费的PDF全文 |
|
