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ABSTRACT:
SUBMITTER: Park MS
PROVIDER: S-EPMC7144182 | biostudies-literature | 2020 Dec
REPOSITORIES: biostudies-literature
Park Myoung-Soon MS Park Hyun-Ju HJ An Young Jae YJ Choi Joon Hun JH Cha Geunyoung G Lee Hwa Jeong HJ Park So-Jung SJ Dewang Purushottam M PM Kim Dae-Kee DK
Journal of enzyme inhibition and medicinal chemistry 20201201 1
A series of 2,4-disubstituted-5-(6-alkylpyridin-2-yl)-1<i>H</i>-imidazoles, <b>7a-c</b>, <b>11a-h</b>, and <b>16a-h</b> has been synthesised and evaluated for their ALK5 inhibitory activity in an enzyme assay and in a cell-based luciferase reporter assay. Incorporation of a quinoxalin-6-yl moiety and a methylene linker at the 4- and 2-position of the imidazole ring, respectively, and a <i>m-</i>CONH<sub>2</sub> substituent in the phenyl ring generated a highly potent and selective ALK5 inhibitor ...[more]