Synthesis and Biological Evaluation of Novel 4(5)-(6-alkylpyridin-2-yl)imidazoles as Inhibitors of Transforming Growth Factor β1 Type Ⅰ Receptor

Abstract

4(5)-(6-Alkylpyridin-2-yl)imidazoles 계열의 신규화합물을 합성하고 이들의 ALK5 저해능을 luciferase reporter을 이용하여 측정하였다. 가장 강력한 저해능을 보인 화합물 7e는 0.1 μM 농도에서 p3TP-Luciferase, SBE-Luciferase, ARE-Luciferase를 각각 93%, 75%, 87%을 저해하며, 같은 농도에서, 각각 31%, 32%, 0%의 저해능을 보인 영국 GSK제약 회사의 SB-431542보다 우수한 화합물임을 입증하였다.;A series of 4(5)-(6-alkylpyridin-2-yl)imidazoles have been synthesized and evaluated for their ALK5 inhibitory activity in the luciferase reporter assays. Compound 7e showed the most significant ALK5 inhibition (p3TP-Luciferase, 93%; SBE-Luciferase, 75%; ARE-Luciferase, 87%) at a concentration of 0.1 μM that is much higher than that of SB-431542 (p3TP-Luciferase, 31%; SBE-Luciferase, 32%; ARE-Luciferase, 0%).