Faculty of Chemistry, Nicolaus Copernicus University, Gagarina 7, 87-100 Toruń, Poland.
J Inorg Biochem. 2012 Oct;115:100-5. doi: 10.1016/j.jinorgbio.2012.05.005. Epub 2012 May 23.
To compare the in vitro cytotoxicity of platinum(II) complexes with 5,7-ditertbutyl-1,2,4-triazolo[1,5-a]pyrimidine (dbtp), three complexes were prepared: cis-[PtI(2)(dbtp)(2)] (1), cis-[Pt(NO(3))(2)(dbtp)(2)] (2) and cis-[Pt(C(4)H(4)O(5))(dbtp)(2)] (3). The coordination compounds have been structurally characterized by IR; (1)H, (13)C, (15)N, (195)Pt NMR and single-crystal X-ray diffraction (1). Spectroscopic studies reveal the monodentate coordination of the heterocycle ligand (dbtp) via N(3) to platinum(II) ions. In addition, the crystal structure of (1) shows that the platinum(II) ion is located in nearly square-planar PtI(2)N(2) environments with two heterocycle ligands (dbtp) arranged in a head-to-head orientation. The complexes have been screened for their cytotoxicity against two human cells: non-small cell lung carcinoma (A549) and breast cancer (T47D). All of the complexes demonstrated a significant antiproliferative activity against both cell lines. On the basis of these results, it is concluded that the cytotoxicity of the studied compounds against T47D follows the order: (3)<(1)<(2).
为了比较 5,7-二叔丁基-1,2,4-三唑并[1,5-a]嘧啶（dbtp）与铂（II）配合物的体外细胞毒性，合成了三种配合物：顺-[PtI2(dbtp)2]（1）、顺-[Pt(NO3)2(dbtp)2]（2）和顺-[Pt(C4H4O5)(dbtp)2]（3）。通过红外光谱（IR）、（1）H、（13）C、（15）N、（195）Pt NMR 和单晶 X 射线衍射（1）对配位化合物进行了结构表征。光谱研究表明，杂环配体（dbtp）通过 N（3）以单齿配位方式与铂（II）离子配位。此外，（1）的晶体结构表明，铂（II）离子位于近乎正方形平面的 PtI2N2 环境中，两个杂环配体（dbtp）呈头对头排列。对这些配合物进行了针对两种人类细胞（非小细胞肺癌（A549）和乳腺癌（T47D））的细胞毒性筛选。所有配合物均对两种细胞系表现出显著的抗增殖活性。基于这些结果，可以得出结论，研究化合物对 T47D 的细胞毒性遵循以下顺序：（3）<（1）<（2）。
