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공영대,천혜경,이태호,강남숙 대한화학회 2010 Bulletin of the Korean Chemical Society Vol.31 No.12
We screened 10,000 heterocyclic small molecules and identified a novel hit core skeleton of 3-(8-chloro-6-(trifluoromethyl)imidazo[1,2-a]pyridine-2-yl)phenyl acetate derivatives. It has been selected as a potential glucagon-like peptide 1 receptor (GLP-1R) activator and demonstrated its effects in increasing GLP-1 secretion, and thereby increasing the glucose responsiveness in both in vitro and pharmacology analyses. Further studies are currently underway to optimize the potency and selectivity of 3-(8-chloro-6-(trifluoromethyl)imidazo[1,2-a]pyridine-2-yl)phenyl acetate derivatives (hit compounds 2 and 8), and address their in vivo efficacy and therapeutic potential. These molecules may serve as useful evidence showing that compounds with a 3-(8-chloro-6-(trifluoromethyl)imidazo[1,2-a]pyridine- 2-yl)phenyl acetate moiety are selective GLP-1R agonists, and have potential as anti-diabetic treatment agents.
공영대 한국공업화학회 2017 한국공업화학회 연구논문 초록집 Vol.2017 No.1
The fused 5 or 6-member heterocyclic compounds offer a high degree of structural diversity and have proven to be broadly useful as therapeutic agents. In this respect, various approaches for these privileged structures with drug-like properties have been developed on solid-phase strategies with druggable design concept. In this symposium, my presentation covers several examples of the finding process of drug-like anti-cancer heterocyclic lead compounds through a key solid supported intermediate based on combinatorial synthetic technology. Some 5 or 6-membered core skeletons showed good anti-cancer activities toward various cancer targets. And then, I will mention about their pharmacological activities of a quinoxaline lead compound toward a novel anti-cancer target for new drug discovery.