Synthesis and biological activity of new bispyridinium salts of 4,4'-bispyridyl-5,5'-perfluoroalkyl-2,2'-bisoxazoles

Eur J Med Chem. 2011 Nov;46(11):5662-7. doi: 10.1016/j.ejmech.2011.09.046. Epub 2011 Oct 2.

Abstract

A series of bispyridinium compounds were synthesized by a short sequence of reactions from symmetric diamides. All compounds were tested for their antiproliferative activity against HT-29, a cell line derived from a human colon adenocarcinoma, and their inhibitory activity against choline kinase (ChoK), a novel anticancer molecular target already in clinical trials. Most of the compounds analyzed showed good antiproliferative activities, in the micromolar range, with the identification of promising lead molecules as a new family of potential inhibitors of ChoK.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Cell Proliferation / drug effects
  • Chemistry Techniques, Synthetic*
  • Choline Kinase / antagonists & inhibitors
  • Electron Transport
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology
  • HT29 Cells
  • Humans
  • Inhibitory Concentration 50
  • Oxazoles / chemical synthesis
  • Oxazoles / chemistry*
  • Oxazoles / pharmacology*
  • Pyridines / chemistry*
  • Salts / chemistry*

Substances

  • Antineoplastic Agents
  • Enzyme Inhibitors
  • Oxazoles
  • Pyridines
  • Salts
  • Choline Kinase
  • pyridine