Affiliation: Second University of Naples
Di Mola A, Peduto A, La Gatta A, Delang L, Pastorino B, Neyts J, et al
. Structure-activity relationship study of arbidol derivatives as inhibitors of chikungunya virus replication. Bioorg Med Chem. 2014;22:6014-25 pubmed publisher
..2 and 14.6, respectively, higher than that of ARB (4.6). ..
Filosa R, Peduto A, Schaible A, Krauth V, Weinigel C, Barz D, et al
. Novel series of benzoquinones with high potency against 5-lipoxygenase in human polymorphonuclear leukocytes. Eur J Med Chem. 2015;94:132-9 pubmed publisher
..Together, our detailed SAR study reveals 22c as highly potent 5-LO-selective lead compound in intact cells that warrants further preclinical evaluation as anti-inflammatory agent. ..
Peduto A, Krauth V, Collarile S, Dehm F, Ambruosi M, Belardo C, et al
. Exploring the role of chloro and methyl substitutions in 2-phenylthiomethyl-benzoindole derivatives for 5-LOX enzyme inhibition. Eur J Med Chem. 2016;108:466-475 pubmed publisher
..The reported inÂ vivo analysis, together with the accessible synthetic procedure, stimulate for the generation of further potent antinflammatory benzoindoles-based agents. ..
Schaible A, Filosa R, Krauth V, Temml V, Pace S, Garscha U, et al
. The 5-lipoxygenase inhibitor RF-22c potently suppresses leukotriene biosynthesis in cellulo and blocks bronchoconstriction and inflammation in vivo. Biochem Pharmacol. 2016;112:60-71 pubmed publisher
Di Mola A, Gatta E, Petronzi C, Cupello A, de Caprariis P, Robello M, et al
. Synthesis and pharmacological evaluation of functionalized isoindolinones on GABA-activated chloride currents in rat cerebellum granule cells in culture. Bioorg Med Chem Lett. 2016;26:5284-5289 pubmed publisher
Zappavigna S, Scuotto M, Cossu A, Ingrosso D, De Rosa M, Schiraldi C, et al
. The 1,4 benzoquinone-featured 5-lipoxygenase inhibitor RF-Id induces apoptotic death through downregulation of IAPs in human glioblastoma cells. J Exp Clin Cancer Res. 2016;35:167 pubmed
..RF-Id induced a caspase-dependent apoptosis in GBM cells by inhibiting IAP family proteins and NFÎºB pathway and represents a promising lead compound for designing a new class of anti-cancer drugs with multiple targets. ..
Peduto A, Scuotto M, Krauth V, Roviezzo F, Rossi A, Temml V, et al
. Optimization of benzoquinone and hydroquinone derivatives as potent inhibitors of human 5-lipoxygenase. Eur J Med Chem. 2017;127:715-726 pubmed publisher
..Together, we elucidated the optimal alkyl chain pattern of quinones and corresponding hydroquinones and reveal a series of highly potent 5-LO inhibitors with effectiveness in vivo that might be useful as anti-inflammatory drugs. ..
Scuotto M, Abdelnabi R, Collarile S, Schiraldi C, Delang L, Massa A, et al
. Discovery of novel multi-target indole-based derivatives as potent and selective inhibitors of chikungunya virus replication. Bioorg Med Chem. 2017;25:327-337 pubmed publisher
..The reported computational insights, together with the accessible synthetic procedure, pave the road towards the design of novel synthetic derivatives with enhanced anti-viral activities. ..
D Agostino A, Stellavato A, Corsuto L, Diana P, Filosa R, La Gatta A, et al
. Is molecular size a discriminating factor in hyaluronan interaction with human cells?. Carbohydr Polym. 2017;157:21-30 pubmed publisher
..Finally our outcomes showed that the lower the fragment size the higher the concern for inflammatory cytokines up-regulation; repair process impairment was highlighted only for 6kDa chains. ..