Targeting the DNA-topoisomerase complex in a double-strike approach with a topoisomerase inhibiting moiety and covalent DNA binder

Chem Commun (Camb). 2012 May 18;48(40):4839-41. doi: 10.1039/c2cc31040f. Epub 2012 Apr 12.

Abstract

Ru(II)(arene)-flavonoids with high in vitro antitumour activity were synthesised. These compounds are capable of inhibiting human topoisomerase IIα and binding covalently to DNA.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antigens, Neoplasm / metabolism*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Coordination Complexes / chemistry
  • Coordination Complexes / pharmacology
  • DNA / metabolism*
  • DNA Topoisomerases, Type II / metabolism*
  • DNA-Binding Proteins / antagonists & inhibitors
  • DNA-Binding Proteins / metabolism*
  • Flavonoids / chemistry
  • Humans
  • Molecular Conformation
  • Protein Binding
  • Ruthenium / chemistry

Substances

  • Antigens, Neoplasm
  • Antineoplastic Agents
  • Coordination Complexes
  • DNA-Binding Proteins
  • Flavonoids
  • Ruthenium
  • DNA
  • DNA Topoisomerases, Type II