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.
出处
《无机化学学报》
SCIE
CAS
CSCD
北大核心
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
