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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Bibliographic Details
Published in:	ACS medicinal chemistry letters Vol. 8; no. 4; pp. 423 - 427
Main Authors:	Hutchinson, John H, Rowbottom, Martin W, Lonergan, David, Darlington, Janice, Prodanovich, Pat, King, Christopher D, Evans, Jilly F, Bain, Gretchen
Format:	Journal Article
Language:	English
Published:	United States American Chemical Society 13-04-2017
Subjects:	Letter lysyl oxidase-like 2 fibrosis inhibitor (2-chloropyridin-4-yl)methanamine LOXL2
Online Access:	Get full text
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Summary:	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.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	1948-5875 1948-5875
DOI:	10.1021/acsmedchemlett.7b00014