Synthesis and in vitro cytotoxicity of novel hydrophilic chiral 2-alkoxy-1,4-butanediamine platinum (II) complexes

Twenty-six new hydrophilic chiral 2-alkoxy-1,4-butanediamine platinum (II) complexes having a seven-membered ring structure between a bidentate carrier ligand and a platinum atom have been synthesized and most of them were evaluated for their in vitro cytotoxicity toward A549 human non-small cell lung carcinoma and HCT-116 human colon cancer cell lines. The cytotoxicities of platinum complexes are related to the nature of the carrier ligand and leaving group. Complex 5′b, viz. cis-dichloro[(2R)-ethoxy-1,4-butanediamine] platinum (II), exhibits the greatest potency among those 21 tested platinum complexes in both cell lines.

Graphical abstractTwenty-six new hydrophilic chiral 2-alkoxy-1,4-butanediamine platinum (II) complexes have been synthesized and most of them were evaluated for their in vitro cytotoxicity toward two human tumor cell lines. The cytotoxicities of platinum complexes are related to the nature of the carrier ligand and leaving group. Complex 5′b exhibits the greatest potency among those 21 tested platinum complexes in both cell lines.Figure optionsDownload full-size imageDownload as PowerPoint slide