Synthesis, characterization and in vitro pharmacological evaluation of new water soluble Ni(II) complexes of 4N-substituted thiosemicarbazones of 2-oxo-1,2-dihydroquinoline-3-carbaldehyde

Eur J Med Chem. 2013 Jun:64:179-89. doi: 10.1016/j.ejmech.2013.03.059. Epub 2013 Apr 6.

Abstract

Four new Ni(II) complexes of general formula [Ni(H2-Qtsc-R)2](NO3)2 (H2-Qtsc-R = 4N-substituted thiosemicarbazones of 2-oxo-1,2-dihydroquinoline-3-carbaldehyde, where R = H (1), Me (2), Et (3), or Ph (4)) have been synthesized and characterized. The geometry of the complexes was confirmed by single crystal X-ray crystallography for one of the complexes (3). The binding affinity of the complexes with DNA and protein have been studied which indicate that they could interact with calf thymus DNA and bovine serum albumin protein. Investigations of antioxidative properties showed that all the complexes have strong radical scavenging properties. Cytotoxic studies showed that the complexes exhibited effective cytotoxic activity against a panel of human cancer cells without affecting the normal cells much.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Antioxidants / chemical synthesis
  • Antioxidants / chemistry
  • Antioxidants / pharmacology*
  • Cattle
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Coordination Complexes / chemistry*
  • Crystallography, X-Ray
  • DNA / chemistry
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • HeLa Cells
  • Hep G2 Cells
  • Humans
  • Mice
  • Models, Molecular
  • Molecular Structure
  • NIH 3T3 Cells
  • Nickel / chemistry*
  • Organometallic Compounds / chemical synthesis
  • Organometallic Compounds / chemistry
  • Organometallic Compounds / pharmacology*
  • Serum Albumin, Bovine / chemistry
  • Solubility
  • Structure-Activity Relationship
  • Thiosemicarbazones / chemistry*
  • Water / chemistry

Substances

  • Antineoplastic Agents
  • Antioxidants
  • Coordination Complexes
  • Organometallic Compounds
  • Thiosemicarbazones
  • Water
  • Serum Albumin, Bovine
  • Nickel
  • DNA
  • calf thymus DNA