Cytotoxic and proapoptotic effects of new Pd(II) and Pt(II)-complexes with 3-ethanimidoyl-2-methoxy-2H-1,2-benzoxaphosphinin-4-ol-2-oxide

Pol J Pharmacol. 2004 Jul-Aug;56(4):473-8.

Abstract

The new palladium (II) and platinum (II) complexes 2 and 3 with 3-ethanimidoyl-2-methoxy-2H-1,2-benzoxaphospinin-4-ol-2-oxide 1 were synthesized and their physicochemical and pharmacological properties were determined. The cytotoxic effects of these complexes were examined on the two human leukemia cell lines, HL-60 and NALM-6. Pd-complex 2 and Pt-complex 3 exerted significant cytotoxic activity. The effects exhibited by these two complexes were comparable to those reported for cis-platin and carboplatin. On the other hand, ligand 1 was not cytotoxic. As determined by caspase-3 activity assay, compounds 2 and 3 differed slightly in their mode of induction of the programmed cell death.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects*
  • Caspase 3
  • Caspases / metabolism
  • Cell Line, Tumor
  • Drug Screening Assays, Antitumor
  • Enzyme Induction
  • Humans
  • Imides / chemistry
  • Imides / pharmacology*
  • Molecular Structure
  • Organometallic Compounds / chemistry
  • Organometallic Compounds / pharmacology*
  • Organophosphorus Compounds / chemistry
  • Organophosphorus Compounds / pharmacology*
  • Organoplatinum Compounds / chemistry
  • Organoplatinum Compounds / pharmacology
  • Palladium*
  • Platinum*
  • Time Factors

Substances

  • 3-ethanimidoyl-2-methoxy-2H-1,2-benzoxaphospinin-4-ol-2-oxide
  • Antineoplastic Agents
  • Imides
  • Organometallic Compounds
  • Organophosphorus Compounds
  • Organoplatinum Compounds
  • Platinum
  • Palladium
  • CASP3 protein, human
  • Caspase 3
  • Caspases