A platinum(IV)-based metallointercalator: synthesis, cytotoxicity, and redox reactions with thiol-containing compounds

作者：Liang Beibei; Huo Shuying^*; Ren Yanli; Sun Shaojing; Cao Ziqing; Shen Shigang

来源：Transition Metal Chemistry, 2015, 40(1): 31-37.

DOI：10.1007/s11243-014-9886-x

A Pt(IV)-based metallointercalator, trans-dichloro(1,10-phenanthroline)(ethylenediamine)platinum(IV) trans-[PtCl2(phen)(en)]Cl-2, was synthesized and characterized by H-1 NMR, ESI-MS, and elemental analysis. Three human carcinoma cell lines Hela, MCF-7, and A549 were employed for in vitro cytotoxicity evaluations using the standard MTT assay. Based on the measured IC50 values, the cytotoxicity of this metallointercalator is very similar to that of cisplatin. Reduction of trans-[PtCl2(phen)(en)](2+) by l-glutathione and 3,6-dioxa-1,8-octanedithiol was studied by H-1 NMR and ESI-MS; the Pt(IV) complex was reduced to its Pt(II) counterpart. The oxidation products of l-glutathione and 3,6-dioxa-1,8-octanedithiol were identified as the glutathione disulfide and the cyclic intramolecular disulfide, respectively. Mechanisms for these reductions are proposed.

• 出版日期2015-2
• 单位河北大学