ml7b00014_si_001.pdf (457.99 kB)
Small Molecule Lysyl Oxidase-like 2 (LOXL2) Inhibitors: The Identification of an Inhibitor Selective for LOXL2 over LOX
journal contribution
posted on 2017-03-01, 00:00 authored by John H. Hutchinson, Martin W. Rowbottom, David Lonergan, Janice Darlington, Pat Prodanovich, Christopher D. King, Jilly F. Evans, Gretchen BainTwo 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.