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Synthesis and Biological Evaluation of Novel 2-Pyridyl Substituted 1,2,3-Triazole Derivatives as Inhibitors of Transforming Growth Fractor-β TypeⅠReceptor

Title
Synthesis and Biological Evaluation of Novel 2-Pyridyl Substituted 1,2,3-Triazole Derivatives as Inhibitors of Transforming Growth Fractor-β TypeⅠReceptor
Authors
Li, Fei
Issue Date
2010
Department/Major
대학원 생명·약학부약학전공
Publisher
이화여자대학교 대학원
Degree
Master
Advisors
유재상
Abstract
Transforming growth factor-β (TGF-β) 신호 전달은 주로 ALK5/smad2/3 pathway를 통하여 이루어지고 있다. TGF-β 신호 전달의 저해는 피부 상처의 재구성을 촉진시키고 흉터의 섬유화를 억제할 것으로 예상된다. TGF-β 신호 전달의 효과적인 저해 전략을 세우기 위해서는 복잡한 TGF-β 신호 전달의 확실한 이론 정립이 필요하다. 본 연구에서는 triazole 유도체들의 합성하였고, p3TP-Lux assay를 통하여 ALK5 inhibition activity를 확인하였다. 합성한 화합물 가운데 화합물 2 (p3TP-Lux, 21%), 화합물 12a (p3TP-Lux, 6%)의 ALK5 inhibition activity를 측정하였고, 이 두 화합물이 ALK5 저해에 효과가 있음을 확인할 수 있었다.;The transforming growth factor-β (TGF-β) signaling is mainly transduced through the ALK5/smad2/3 pathway. Inhibition of TGF-β signaling would be predicted to enhance re-epthelialization of cutaneous wound and reduce scarring fibrosis. For determining an effective anti-TGF-β strategy for fibrosis, it is necessary to investigate the complex signaling of TGF-β. In this study, we synthesized a series of triazole analogues and evaluated their ALK5 inhibitory activity in p3TP-Lux assays. The compound 2 (p3TP-Lux, 21%), and 12a (p3TP-Lux, 6%) showed an inhibitory activity against ALK5.
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일반대학원 > 생명·약학부 > Theses_Master
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