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ID: ALA1148859
Journal: Bioorg Med Chem Lett
Title: A new 4-(2-methylquinolin-4-ylmethyl)phenyl P1' group for the beta-amino hydroxamic acid derived TACE inhibitors.
Authors: Chen XT, Ghavimi B, Corbett RL, Xue CB, Liu RQ, Covington MB, Qian M, Vaddi KG, Christ DD, Hartman KD, Ribadeneira MD, Trzaskos JM, Newton RC, Decicco CP, Duan JJ.
Abstract: A new P1' group for TACE inhibitors was identified by eliminating the oxygen atom in the linker of the original 4-(2-methylquinolin-4-ylmethoxy)phenyl P1' group. Incorporation of this 4-(2-methylquinolin-4-ylmethyl)phenyl group onto different beta-aminohydroxamic acid cores provided compound 18, which demonstrated potent porcine TACE (p-TACE) and human whole blood activity, excellent PK properties, and good selectivity against a variety of MMPs.
CiteXplore: 17276676