Synthesis, biological evaluation and DNA binding properties of novel mono and bisnaphthalimides

Org Biomol Chem. 2003 Feb 21;1(4):648-54. doi: 10.1039/b209042b.

Abstract

A novel series of mono and bisnaphthalimides was synthesized and their antiproliferative activities were evaluated against three tumor cell lines. Bisnaphthalimides 3 and 4, bearing a pyrazine ring fused to the naphthalimide system, showed activities in the order of 10(-8) microM, similar to elinafide. DNA binding properties and the ability to induce DNA damage were studied for some of the most active compounds.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology
  • Cell Division / drug effects
  • Cell Line, Tumor
  • Comet Assay
  • DNA / chemistry*
  • DNA Damage
  • Humans
  • Intercalating Agents / chemical synthesis
  • Intercalating Agents / pharmacology
  • Naphthalenes / chemical synthesis*
  • Naphthalenes / chemistry
  • Naphthalenes / pharmacology*
  • Structure-Activity Relationship
  • Topoisomerase I Inhibitors
  • Topoisomerase II Inhibitors

Substances

  • Antineoplastic Agents
  • Intercalating Agents
  • Naphthalenes
  • Topoisomerase I Inhibitors
  • Topoisomerase II Inhibitors
  • DNA