[NiII(3-OMe-salophene)]: a potent agent with antitumor activity

J Med Chem. 2010 Aug 26;53(16):6064-70. doi: 10.1021/jm100459k.

Abstract

In this study, we investigated the anticancer properties of methoxy-substituted nickel(II)(salophene) derivatives. We demonstrated that the most active complex [NiII(3-OMe-salophene)] is not necrotic in Burkitt-like lymphoma cells (BJAB) and human B-cell precursor cells (Nalm-6). [NiII(3-OMe-salophene)] inhibited proliferation and induced apoptosis in a concentration dependent manner, giving evidence for the involvement of CD95 receptor-mediated, extrinsic pathway. Furthermore, [NiII(3-OMe-salophene)] overcame vincristine drug resistance in BJAB and Nalm-6 cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Apoptosis / drug effects
  • Apoptosis Regulatory Proteins
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Coordination Complexes / chemical synthesis*
  • Coordination Complexes / chemistry
  • Coordination Complexes / pharmacology
  • Drug Resistance, Neoplasm / drug effects
  • Drug Screening Assays, Antitumor
  • Fas-Associated Death Domain Protein / biosynthesis
  • Humans
  • Intracellular Signaling Peptides and Proteins
  • Magnetic Resonance Spectroscopy
  • Mitochondrial Proteins / biosynthesis
  • Necrosis
  • Signal Transduction
  • Structure-Activity Relationship
  • Vincristine / pharmacology
  • fas Receptor / physiology

Substances

  • Antineoplastic Agents
  • Apoptosis Regulatory Proteins
  • Coordination Complexes
  • DIABLO protein, human
  • Fas-Associated Death Domain Protein
  • Intracellular Signaling Peptides and Proteins
  • Mitochondrial Proteins
  • fas Receptor
  • Vincristine