（（R）-（-）-1,2-丙二胺）（1,3-丙二酸）合铂（II）的合成、表征及抗肿瘤活性研究

贵金属, 2014, (4): 26-29.

（（R）-（-）-1,2-丙二胺）（1,3-丙二酸）合铂（II）的合成、表征及抗肿瘤活性研究

丛艳伟 ^1, , 陈宏 ^2, , 栾春芳 ^3, , 白炘劼 ^4, , 普绍平 ^5,

1.昆明贵研药业有限公司,昆明,650106

2.昆明贵研药业有限公司，昆明 650106; 昆明贵金属研究所，昆明 650106

3.昆明贵研药业有限公司,昆明,650106

4.昆明贵研药业有限公司,昆明,650106

5.昆明贵研药业有限公司,昆明,650106

基金项目: 昆明市重点科技计划项目(昆科计字2012-03-01-B-H-04-0006)。

关键词：药物化恘 , 1,2-丙二胺 , 铂配合物 , 合成 , 表征 , 抗肿瘤活性

Synthesis, Characterization and Anticancer Activity of ((R)-(-)-1,2-diaminepropane)(1,3-malonate) Platinum(II)

Keywords： medicinal chemistry , 1,2-diaminepropane , platinum complex , synthesis , characterization , antitcancer activity

以1,2-丙二胺为起始原料，经手性拆分得到R-(-)-1,2-丙二胺，再同氯亚铂酸钾、碘化钾、硝酸银、1,3-丙二酸钠等物质反应，制成((R)-(-)-1,2-丙二胺)(1,3-丙二酸)合铂(II)，通过元素分析、红外光谱、核磁共振等对其进行化恘结构确证，结果表明所合成产品同理论一致，并进行初步体外活性评价，表明该化合物对于肺癌A-549及白血病HL-60肿瘤细胞有一定活性。

(R)-(-)-1,2diaminepropane was obtained by rotation resolution of 1,2-diaminepropane as the starting material, and then was reacted with potassium tetrachloroplatinate, potassium iodide, silver nitrate, sodium 1,3-malonate to produce ((R)-(-)-1,2-diaminepropane)(1,3-malonate) platinum(II). Elemental analysis, infrared and nuclear magnetic resonance were used to characterize its chemical structure. Preliminary in vitro anticancer test showed that the complex was active against A-549 and HL-60 cancer cell line.

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