Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1377757 | Bioorganic & Medicinal Chemistry Letters | 2007 | 6 Pages |
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 β-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.
Graphical abstractA 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. The synthesis and profile of TACE inhibitor (18) was described.Figure optionsDownload full-size imageDownload as PowerPoint slide