Synthesis and biological evaluation of platinum(II) complexes containing (1R,2R)-N1-alkyl-1,2-diaminocyclohexane and D-(+)-camphorate ligands

Five platinum(II) complexes with N-monoalkyl derivatives of 1R,2R-diaminocyclohexane as ligands and D-(+)-camphorate anion as leaving group have been synthesized and characterized by elemental analysis, IR, 1H NMR, ESI-MS, and HRMS spectra. All complexes were evaluated for their in vitro cytotoxicity against four human tumor cell lines and most of them showed promising cytotoxic activity, especially compounds 3 and 4 with branched alkyl substituent at one of nitrogen atoms. Preliminary mechanism study by flow cytometry and agarose gel electrophoresis was also carried out in comparison with cisplatin and oxaliplatin.

Five platinum(II) complexes with (1R,2R)-N1-alkyl-1,2-diaminocyclohexane and D-(+)-camphorate ligands were synthesized, characterized and evaluated for their in vitro antitumor activities against four cancer cell lines, and preliminary mechanism study by flow cytometry and agarose gel electrophoresis was also carried out.Figure optionsDownload as PowerPoint slideHighlights
► Five platinum(II) complexes with (1R,2R)-N1-alkyl-1,2-diaminocyclohexane and D-(+)-camphorate ligands.
► Most of complexes showed in vitro cytotoxicity against four tumor cell lines.
► DNA synthesis phase in cell cycle was the target of drugs.
► DNA unwinding effect of typical compounds was observed.