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.
Sang-sup Jew  1 ,  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
Affiliations
  • 1. Research Institute of Pharmaceutical Sciences and College of Pharmacy, Seoul National University, Seoul 151-742, South Korea. [email protected]
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.