Synthesis and cytotoxicity of diam(m)ineplatinum(II) complexes with 2,2-bis(hydroxymethyl)malonate as the leaving group

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• 作者：Yingjuan Xing^a ; Liguang Lou^b ; Xizhu Chen^a ; Qingsong Ye^a ; Yongping Xu^b ; Chengying Xie^b ; Jing Jiang^a ; Weiping Liu^a ; ^{liuweiping0917@126.com}
• 关键词：Platinum ; 2 ; 2-bis(Hydroxymethyl)malonate ; Synthesis ; Anticancer activity
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 March, 2012
• 卷：22
• 期：6
• 页码：2239-2241
• 文件大小：267 K

摘要

Six diam(m)ineplatinum(II) complexes with 2,2-bis(hydroxymethyl)malonate as the leaving group were synthesized and characterized by elemental analysis, FAB-MS, FT-IR, ¹H and ¹³C NMR along with a single crystal X-ray diffraction for a representative compound. All the complexes were evaluated for the cytotoxicity against human cancer cell lines A549/ATCC, HT-29, SGC-7901. The activity is related to the nature of the am(m)ine ligand. cis-[Pt(II)(1R,2R-Diaminocyclohexane)路2,2-bis(hydroxymethyl)malonate] (complex 5) exhibits the greatest activity among those six complexes, and is even more active than its parent compound oxaliplatin. LD₅₀ was found to be 115 mg/kg by iv administration to ICR mice, much larger than that of oxaliplatin (LD₅₀ = 19 mg/kg).