Design of a platinum-acridine-endoxifen conjugate targeted at hormone-dependent breast cancer

Chem Commun (Camb). 2013 Mar 25;49(24):2415-7. doi: 10.1039/c3cc38957j.

Abstract

The synthesis of a novel pharmacophore comprising a DNA-targeted platinum-acridine hybrid agent and estrogen receptor-targeted 4-hydroxy-N-desmethyltamoxifen (endoxifen) using carbamate coupling chemistry and its evaluation in breast cancer cell lines are described.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acridines / chemistry*
  • Antineoplastic Agents, Hormonal / chemistry*
  • Antineoplastic Agents, Hormonal / therapeutic use
  • Antineoplastic Agents, Hormonal / toxicity
  • Breast Neoplasms / drug therapy
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • DNA / chemistry
  • DNA / metabolism
  • Drug Design*
  • Female
  • Humans
  • Intercalating Agents / chemistry
  • Intercalating Agents / therapeutic use
  • Intercalating Agents / toxicity
  • MCF-7 Cells
  • Platinum / chemistry*
  • Receptors, Estrogen / antagonists & inhibitors
  • Receptors, Estrogen / metabolism
  • Tamoxifen / analogs & derivatives*
  • Tamoxifen / chemistry

Substances

  • Acridines
  • Antineoplastic Agents, Hormonal
  • Intercalating Agents
  • Receptors, Estrogen
  • Tamoxifen
  • 4-hydroxy-N-desmethyltamoxifen
  • Platinum
  • DNA