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.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
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 )~~
