Small Molecule Lysyl Oxidase-like 2 (LOXL2) Inhibitors: The Identification of an Inhibitor Selective for LOXL2 over LOX

Small Molecule Lysyl Oxidase-like 2 (LOXL2) Inhibitors: The Identification of an Inhibitor Selective for LOXL2 over LOX

Two series of novel LOXL2 enzyme inhibitors are described: benzylamines substituted with electron withdrawing groups at the para-position and 2-substituted pyridine-4-ylmethanamines. The most potent compound, (2-chloropyridin-4-yl)­methanamine 20 (hLOXL2 IC50 = 126 nM), was shown to be selective for...

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Veröffentlicht in:ACS medicinal chemistry letters 2017-04, Vol.8 (4), p.423-427
Hauptverfasser: Hutchinson, John H, Rowbottom, Martin W, Lonergan, David, Darlington, Janice, Prodanovich, Pat, King, Christopher D, Evans, Jilly F, Bain, Gretchen
Format: Artikel
Sprache:eng
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Letter
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Zusammenfassung:Two series of novel LOXL2 enzyme inhibitors are described: benzylamines substituted with electron withdrawing groups at the para-position and 2-substituted pyridine-4-ylmethanamines. The most potent compound, (2-chloropyridin-4-yl)­methanamine 20 (hLOXL2 IC50 = 126 nM), was shown to be selective for LOXL2 over LOX and three other amine oxidases (MAO-A, MAO-B, and SSAO). Compound 20 is the first published small molecule inhibitor selective for LOXL2 over LOX.
ISSN:1948-5875
1948-5875
DOI:10.1021/acsmedchemlett.7b00014