2-甲氧基乙胺为配体的铂(Ⅱ)配合物的合成及其体外抗肿瘤活性  

Synthesis and Antitumor Activities in vitro of a Series of Platinum(Ⅱ) Complexes with 2-Methoxyethylamine

作　　者：王联红[1,2] 刘芸[3] 袁阜平[3] 尤启冬[1] 苟少华[3] 

机构地区：[1]中国药科大学药学院 [2]南京大学配位化学国家重点实验室,南京210093 [3]南京大学配位化学国家重点实验室

出　　处：《中国药科大学学报》2005年第2期106-110,共5页Journal of China Pharmaceutical University

基　　金：国家自然科学基金资助项目 (No .2 0 4710 2 7) ;江苏省自然科学基金资助项目 (No .BK2 0 0 44 13 )~~

摘　　要：目的:研究以2 甲氧基乙胺为载体配基的铂(II)配合物的合成及其体外抗肿瘤活性。方法:以K2 PtCl4为原料,经多步反应合成目标配合物[(CH3 OCH2 CH2 NH2 ) 2 Pt(II)X2 ](其中X为氯离子、2 甲氧基乙酸根,或X2 =草酸根、丙二酸根、1,1 环丁烷二羧酸根、dl 樟脑酸根和d 樟脑酸根)。测试了w 1、w 2对HL 6 0人白血病细胞、BEL 74 0 2人肝癌细胞的体外抗肿瘤活性;w 3～w 7对A5 4 9人肺癌细胞的体外抗肿瘤活性。结果与结论:目标配合物结构经元素分析、红外光谱、氢核磁共振谱和质谱确证。该系列配合物整体抗肿瘤活性效果一般,但是w 5的相对较好的活性结果暗示离去基团中插入醚键有助于提高铂(II)配合物的抗肿瘤活性。AIM:To study the synthesis and antitumor activiti es in vitro of a series of platinum (II) complexes having 2-methoxyethylamine as carrier ligand.METHOD: Seven novel platinum (II) complexes [Pt(II)A 2X 2](A =2-methoxyethylamine;X=chloride anion,2-methox yacetato,X 2=oxalato,malonato,1,1-cyclobutanedicarboxylato,dl-a nd d-camphorato) have been prepared from K 2PtCl 4.The antitumor activities in vitro of complexes w-1 and w-2 toward HL-60 human leukemia and BEL-7402 human Hepatocarcinoma were evaluated. The antitumor activities in vitro of complexes w-3～w-7 against A549 human lung ca rc inoma cells were also studied.RESULT AND CONCLUSI ON:All the targe t platinum (II) complexes were characterized by elemental analysis,IR, 1H NMR and ESI-MS spectra. Low activity against selected cell lines were sho wn in all the complexes. The relatively good antitumor activity of complex w -5 implied that the incorporation of oxygen in the leaving grou p of the platinum complex could enhance the antitumor activity.

关 键 词：2-甲氧基乙胺 铂(Ⅱ)配合物 合成 抗肿瘤活性 

分 类 号：R914[医药卫生—药物化学] R730.5[医药卫生—药学]