Mononuclear Pd(II) and Pt(II) complexes with an α-N-heterocyclic thiosemicarbazone: cytotoxicity, solution behaviour and interaction versus proven models from biological media,Inorganic Chemistry Frontiers

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Mononuclear Pd(II) and Pt(II) complexes with an α-N-heterocyclic thiosemicarbazone: cytotoxicity, solution behaviour and interaction versus proven models from biological media
Inorganic Chemistry Frontiers ( IF 6.1 ) Pub Date : 2017-10-18 00:00:00 , DOI: 10.1039/c7qi00446j
Ana I. Matesanz _{1,

2,

3} , Eva Jimenez-Faraco _{1,

2,

3} , María C. Ruiz _{4,

5,

6,

7,

8} , Lucia M. Balsa _{4,

5,

6,

7,

8} , Carmen Navarro-Ranninger _{1,

2,

3} , Ignacio E. León _{4,

5,

6,

7,

8} , Adoracion G. Quiroga _{1,

2,

3}

Affiliation

Two Pd(II) and Pt(II) complexes with two pyrrol-2-carbaldehyde N-p-chlorophenylthiosemicarbazone ligands are designed and characterized showing mononuclear structures. An important pharmacological property for both compounds is the high selectivity for tumor cells and a lack of activity in healthy cells. The Pd(II) compound shows a higher antitumor activity and selectivity than the Pt(II) compound. Both complexes present a variety of biological interactions: with DNA models (pBR322 and CT DNA), proteins (lysozyme and RNase) and other biological targets like proteosome. Our results show that the Pd(II) complex is a more interesting candidate for potential anticancer therapies than the Pt(II) complex, and we provide new insight into the design and synthesis of palladium compounds as potential antitumor agents.

中文翻译：

单核Pd（II）和Pt（II）配合物与α-N-杂环硫代半乳糖胺：细胞毒性，溶液行为和相互作用与生物介质的经过验证的模型相比

设计并表征了具有两个吡咯-2-甲醛Np-氯苯基硫代半脲配体的两个Pd（II）和Pt（II）配合物，并显示了单核结构。这两种化合物的重要药理性质是对肿瘤细胞的高选择性以及在健康细胞中缺乏活性。Pd（II）化合物显示出比Pt（II）化合物更高的抗肿瘤活性和选择性。两种复合物都具有多种生物学相互作用：与DNA模型（pBR322和CT DNA），蛋白质（溶菌酶和RNase）以及其他生物靶标（如蛋白体）相互作用。我们的结果表明Pd（II）复合物比Pt（II）复合物更可能成为潜在的抗癌治疗方法，我们为钯化合物作为潜在的抗肿瘤药物的设计和合成提供了新的见识。

更新日期：2017-11-08

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