Complexation with organometallic ruthenium pharmacophores enhances the ability of 4-anilinoquinazolines inducing apoptosis

Chem Commun (Camb). 2013 Nov 11;49(87):10224-6. doi: 10.1039/c3cc43000f.

Abstract

The complexation with organoruthenium fragments confers 4-anilinoquinazoline pharmacophores with higher potential for inducing cellular apoptosis while the highly inhibitory activity of 4-anilinoquinazolines against EGFR and the reactivity of the ruthenium centre to 9-ethylguanine are well preserved.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aniline Compounds / chemistry*
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects*
  • Cell Proliferation / drug effects
  • Crystallography, X-Ray
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • ErbB Receptors / antagonists & inhibitors
  • Humans
  • Hydrolysis
  • MCF-7 Cells
  • Models, Molecular
  • Molecular Structure
  • Organometallic Compounds / chemical synthesis
  • Organometallic Compounds / chemistry
  • Organometallic Compounds / pharmacology*
  • Quinazolines / chemistry*
  • Ruthenium / chemistry*
  • Structure-Activity Relationship

Substances

  • Aniline Compounds
  • Antineoplastic Agents
  • Organometallic Compounds
  • Quinazolines
  • Ruthenium
  • ErbB Receptors