Preparation, characterization, and antitumor activity of new ethylenediamine platinum(IV) complexes containing mixed carboxylate ligands

J Inorg Biochem. 1993 May 1;50(2):79-87. doi: 10.1016/0162-0134(93)80015-2.

Abstract

A series of ethylenediamine platinum(IV) complexes of the type PtIV(en)XA2 and PtIV(en)X'2A2, where X = 1,1-cyclobutanedicarboxylato or malonato, X' = chloro, cyclobutanecarboxylato, cyclopentanecarboxylato, or cyclohexanecarboxylato, and A = acetato or trifluoroacetato were synthesized and characterized by elemental analysis, infrared, and NMR (13C and 195Pt) spectroscopic techniques. These compounds had good to excellent antitumor activity against murine leukemia L1210 cells. Complexes with axial trifluoroacetate groups were superior to those with acetate ligands. Those possessing both axial trifluoroacetate groups and monodentate bis-carboxylate ligands in the equatorial positions were the most active in the series investigated.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / therapeutic use
  • Carboxylic Acids / chemistry*
  • Ethylenediamines / chemical synthesis*
  • Ethylenediamines / chemistry
  • Ethylenediamines / therapeutic use
  • Leukemia L1210 / drug therapy
  • Magnetic Resonance Spectroscopy
  • Mice
  • Molecular Structure
  • Platinum / chemistry*
  • Structure-Activity Relationship
  • Tumor Cells, Cultured

Substances

  • Antineoplastic Agents
  • Carboxylic Acids
  • Ethylenediamines
  • Platinum