Synthesis and biological evaluation of mixed ammine/amine platinum(II) complexes with dicarboxylate containing organic nitrate as ligand

• Two mixed ammine/amine platinum(II) complexes with dicarboxylate containing organic nitrate as ligand.
• Complex 1 shows high in vitro cytotoxicity against A549 and SGC7901.
• The compounds possess DNA unwinding capability similar to cisplatin.

Two novel platinum(II) complexes cis-[Pt(L′)(NH3)X] (where L′ = cyclopentylamine or cyclohexylamine, X = 3-(nitrooxy)cyclobutane-1,1-dicarboxylate) were synthesized and spectrally characterized in this study. The purity of complexes 1 and 2 were studied by HPLC–MS spectra, and the contents of complexes 1 and 2 were more than 98%. It was demonstrated that the newly synthesized compounds with dicarboxylate containing organic nitrate as ligand possessed DNA unwinding capability similar to cisplatin by the means of agarose gel electrophoresis. In addition, the antiproliferative study by WST-8 assay revealed that these platinum(II) complexes exhibited considerable cytotoxicity against tested cancer cell lines in vitro compared with positive agents (cisplatin, oxaliplatin and carboplatin), especially complex 1, showing higher in vitro antitumoractivity than oxaliplatin and carboplatin in SGC7901 and A549 cell lines.

Two mixed ammine/amine platinum(II) complexes with dicarboxylate containing organic nitrate as ligand were synthesized, characterized and evaluated for their in vitro antitumor activities against five cancer cell lines, and the DNA unwinding capability was also investigated.Figure optionsDownload as PowerPoint slide