Quiroga A G, Pérez J M, Montero E I, Masaguer J R, Alonso C, Navarro-Ranninger C
Departamento de Química Inorgánica, Facultad de Ciencias, Universidad Autónoma de Madrid, Spain.
J Inorg Biochem. 1998 May;70(2):117-23. doi: 10.1016/s0162-0134(98)10007-7.
In the present paper we report the synthesis and characterization by 1H 13C NMR and heteronuclear 2D NMR spectroscopies of two new metallic complexes derived from phenylacetaldehyde thiosemincarbazone: Pt(C9H11N3S)Cl2, compound 2, and Pd(C9H11N3S)Cl2, compound 3. The testing of the cytotoxic activity of these compounds against several human and murine cell lines sensitive and resistant to cis-DDP suggests that compounds 2 and 3 may be considered potential anticancer agents since they exhibit 1C50 values in a microM range similar to cisplatin (cis-DDP). The cytotoxic activity of these compounds is higher in cis-DDP-resistant tumor cells than that of other antitumor drugs such as etoposide and adriamycin. On the other hand, the analysis of the interaction of compounds 2 and 3 with linear plasmid DNA indicate that both compounds, particularly compound 3, have an enhanced capacity to form DNA interstrand cross-links in comparison with cis-DDP.
在本论文中，我们报道了由苯乙醛缩氨基硫脲衍生的两种新型金属配合物的合成及其通过1H 13C NMR和异核二维NMR光谱进行的表征：Pt(C9H11N3S)Cl2，化合物2，以及Pd(C9H11N3S)Cl2，化合物3。对这些化合物针对几种对顺铂敏感和耐药的人类及小鼠细胞系的细胞毒性活性测试表明，化合物2和3可被视为潜在的抗癌剂，因为它们表现出的IC50值在与顺铂（顺式-DDP）相似的微摩尔范围内。这些化合物在顺铂耐药肿瘤细胞中的细胞毒性活性高于其他抗肿瘤药物，如依托泊苷和阿霉素。另一方面，对化合物2和3与线性质粒DNA相互作用的分析表明，与顺铂相比，这两种化合物，尤其是化合物3，具有更强的形成DNA链间交联的能力。
