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

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.

• Authors: Sang-sup Jew, Boon-saeng Park, Doo-yeon Lim, Myoung Goo Kim, In Kwon Chung, Joo Hee Kim, Chung Il Hong, Joon-Kyum Kim, Hong-Jun Park, Jun-Hee Lee, Hyeung-geun Park
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 13 Issue 4 Pg. 609-12 (Feb 24 2003) ISSN: 0960-894X [Print] England
• PMID: 12639541 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Enzyme Inhibitors
• Esters
• Pyridines
• Telomerase

Topics

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