title: Synthesis and evaluation of LOX inhibitory activity of 2-(1,3-Dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)-N-phenylacetamide derivatives.
abstract: A family of structurally related LOX enzymes present in human cells which catalyse the metabolism of released arachidonic acid from phospholipids by inflammatory stimuli, to biologically active mediators. Mainly, expression of three types of LOXs occurs in cells, which catalyse the insertion of molecular oxygen into the molecule of arachidonic acid at carbon 5, 12, and 15. According to this chemical reaction, the LOXs are named 5-, 12-, and 15-LOX, amongst which, 15-LOX with isoforms 15-LOX-1 and 15-LOX-2 have critical role in neoplastic diseases. 15-LOX-1 is overexpressed in some neoplastic conditions. Hence, in this research, we focused on the synthesis of naphthalimide analogs as potential 15-LOX-1 inhibitors. Fortunately, the most of synthesized compounds demonstrated remarkable inhibitory potency towards 15-LOX-1 in nanomolar ranges. Naphthalimide derivatives could be suggested as potential LOX inhibitors with likely applications of anticancer activity.
authors.affiliation: Pharmaceutical Sciences Research Center, School of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, I.R. Iran; Department of Pharmacology, Toxicology and Medical Services, School of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, I.R. Iran.
authors.forename: Ahmad
authors.initials: A
authors.lastname: Mohammadi-Farani
authors.affiliation: Students Research Committee, Kermanshah University of Medical Sciences, Kermanshah, I.R. Iran; Department of Medicinal Chemistry, School of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, I.R. Iran.
authors.forename: Arash
authors.initials: A
authors.lastname: Haqiqi
authors.affiliation: Pharmaceutical Sciences Research Center, School of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, I.R. Iran; Department of Pharmacology, Toxicology and Medical Services, School of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, I.R. Iran.
authors.forename: Sahar Jamshidy
authors.initials: SJ
authors.lastname: Navid
authors.affiliation: Pharmaceutical Sciences Research Center, School of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, I.R. Iran; Department of Medicinal Chemistry, School of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, I.R. Iran.
authors.forename: Alireza
authors.initials: A
authors.lastname: Aliabadi
keywords: Arachidonic acid; Lipoxygense; Naphthalimide; Synthesis