Synthesis, characterization, toxicity, cytogenetic and in vivo antitumor studies of 1,1-dithiolate Cu(II) complexes with di-, tri-, tetra- amines and 1,3-thiazoles. Structure-activity correlation

Bioorg Med Chem. 2009 Apr 15;17(8):3142-51. doi: 10.1016/j.bmc.2009.02.059. Epub 2009 Mar 5.

Abstract

A series of new mixed-ligand neutral copper(II) complexes of the general type [Cu(amine)(i-MNT)] and [Cu(tz)(i-MNT)] was prepared and characterized by elemental, spectroscopic methods, mu(eff), Lambda(mu) measurements and molecular modeling studies. The acute toxicity, the cytogenetic and the in vivo antitumor activity of the new complexes, is related to their chemical and physicochemical properties. Among the Cu(II) compounds tested the complex with 2-amino-5-methyl thiazole increases significantly the life span of leukemia P388 bearing mice in vivo.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amines / chemical synthesis
  • Amines / chemistry
  • Amines / pharmacology
  • Animals
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Copper / chemistry*
  • Female
  • Humans
  • Leukemia P388 / drug therapy
  • Ligands
  • Lymphocytes / drug effects
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Mice, Inbred DBA
  • Models, Molecular
  • Organometallic Compounds / chemical synthesis*
  • Organometallic Compounds / chemistry
  • Organometallic Compounds / pharmacology*
  • Sister Chromatid Exchange / drug effects
  • Spectrophotometry, Infrared
  • Structure-Activity Relationship
  • Sulfhydryl Compounds / chemical synthesis
  • Sulfhydryl Compounds / chemistry
  • Sulfhydryl Compounds / pharmacology
  • Thiazoles / chemical synthesis
  • Thiazoles / chemistry
  • Thiazoles / pharmacology

Substances

  • Amines
  • Antineoplastic Agents
  • Ligands
  • Organometallic Compounds
  • Sulfhydryl Compounds
  • Thiazoles
  • Copper