In vitro cytotoxicity study on platinum (II) complexes with epoxysuccinates as leaving groups

Bioorg Med Chem Lett. 2007 Jul 15;17(14):3831-4. doi: 10.1016/j.bmcl.2007.05.014. Epub 2007 May 13.

Abstract

A series of novel cisplatin-type platinum complexes were designed, characteristic of epoxysuccinates as leaving groups. The pertinent compounds were prepared and characterized by IR, (1)H NMR, and ESI-MS spectra with elementary analyses. The in vitro cytotoxic activities of compounds toward SPC-A1 human lung adenocarcinoma cell line and BGC823 human stomach adenocarcinoma cell line were determined. Biological tests have confirmed that complexes containing 4R,5R-DMID [abbreviation of (4R,5R)-4,5-bis (aminomethyl)-2-isopropyl-1,3-dioxolane] as carrier ligands have greater cytotoxicity toward tumor cells than the corresponding compounds with other carrier ligands. Most platinum complexes with trans-epoxysuccinates usually have higher cytotoxicity than those with cis-epoxysuccinates. Complex 4a shows the most effective among those tested platinum complexes in both cell lines, and its cytotoxicity approached that of cisplatin.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenocarcinoma / pathology
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Epoxy Compounds / chemistry*
  • Humans
  • In Vitro Techniques
  • Lung Neoplasms / pathology
  • Magnetic Resonance Spectroscopy
  • Platinum Compounds / chemistry
  • Platinum Compounds / pharmacology*
  • Spectrometry, Mass, Electrospray Ionization
  • Succinates / chemistry*

Substances

  • Antineoplastic Agents
  • Epoxy Compounds
  • Platinum Compounds
  • Succinates