2,6-Dithienyl-4-furyl pyridines: Synthesis, topoisomerase I and II inhibition, cytotoxicity, structure-activity relationship, and docking study

Bioorg Med Chem Lett. 2010 Jan 1;20(1):42-7. doi: 10.1016/j.bmcl.2009.11.041. Epub 2009 Nov 14.

Abstract

For the development of novel antitumor agents, 2,6-dithienyl-4-furyl pyridine derivatives were prepared and evaluated for their topoisomerase I and II inhibitory activity as well as cytotoxicity against several human cancer cell lines. Among the 21 prepared compounds, compound 24 exhibited strong topoisomerase I inhibitory activity. In addition, a docking study with topoisomerase I and compound 24 was performed.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / toxicity
  • Binding Sites
  • Cell Line, Tumor
  • Computer Simulation
  • DNA Topoisomerases, Type I / metabolism*
  • DNA Topoisomerases, Type II / metabolism*
  • Drug Screening Assays, Antitumor
  • Humans
  • Pyridines / chemical synthesis
  • Pyridines / chemistry*
  • Pyridines / toxicity
  • Structure-Activity Relationship
  • Thiophenes / chemical synthesis*
  • Thiophenes / chemistry
  • Thiophenes / toxicity
  • Topoisomerase I Inhibitors
  • Topoisomerase II Inhibitors

Substances

  • Antineoplastic Agents
  • Pyridines
  • Thiophenes
  • Topoisomerase I Inhibitors
  • Topoisomerase II Inhibitors
  • DNA Topoisomerases, Type I
  • DNA Topoisomerases, Type II