Synthesis of 6-formyl-pyridine-2-carboxylate derivatives and their telomerase inhibitory activities.
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.
Jew
Sang-sup
SS
Research Institute of Pharmaceutical Sciences and College of Pharmacy, Seoul National University, Seoul 151-742, South Korea. ssjew@plaza.snu.ac.kr
Park
Boon-saeng
BS
Lim
Doo-yeon
DY
Kim
Myoung Goo
MG
Chung
In Kwon
IK
Kim
Joo Hee
JH
Hong
Chung Il
CI
Kim
Joon-Kyum
JK
Park
Hong-Jun
HJ
Lee
Jun-Hee
JH
Park
Hyeung-geun
HG
D002455:Cell Division / Q000187:drug effects; D045744:Cell Line, Tumor; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D004952:Esters / Q000138:chemical synthesis / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D019098:Telomerase / Q000037:antagonists & inhibitors*
D004791:Enzyme Inhibitors; D004952:Esters; D011725:Pyridines; D019098:Telomerase