Synthesis of 6-formyl-pyridine-2-carboxylate derivatives and their telomerase inhibitory activities

Bioorg Med Chem Lett. 2003 Feb 24;13(4):609-12. doi: 10.1016/s0960-894x(02)01041-7.

Abstract

Twenty-one pyridine-2-carboxylate derivatives were prepared by the coupling of 6-formyl-2-carboxylic acid with the corresponding phenol, thiophenol, and aniline, substituted with various functional groups. Among them, the 3,4-dichlorothiophenol ester (9p) showed the highest in vitro telomerase inhibitory activity and quite significant in vivo tumor suppression activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Division / drug effects
  • Cell Line, Tumor
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / pharmacology
  • Esters / chemical synthesis
  • Esters / pharmacology
  • Humans
  • Inhibitory Concentration 50
  • Pyridines / chemical synthesis*
  • Pyridines / pharmacology
  • Structure-Activity Relationship
  • Telomerase / antagonists & inhibitors*

Substances

  • Enzyme Inhibitors
  • Esters
  • Pyridines
  • Telomerase