Chemical Preparation and Biological Evaluation of Novel Lipophilic Platinum(II) Complexes of Salicylate Derivatives

摘要

A series of novel lipophilic platinum(II) complexes containing salicylate derivatives as the leaving group were synthesized and characterized by elemental analysis, FAB~+-MS, FT-IR and ~1H NMR spectroscopy. The chemical structural parameters were also calculated using DFT (B3LYP). Most of the resulting platinum complexes exhibited high solubility in organic solvents such as ethanol, acetone and ether, and had right partition coefficient suited to be encapsulated in liposomes. The pertinent complexes were evaluated for their in vitro cytotoxicity against A549 human lung carcinoma and SGC-7901 human gastric carcinoma cell lines, and for the in vivo antitumor activity on S180 or non-small cell lung tumors of mice. Two of the complexes, Compound 6 and 8, were found to be more active and less toxic than carboplatin and oxaliplatin, showing great potential to be developed as anticancer agents.