61854-89-5Relevant articles and documents
Synthesis, structure, and antioxidant activity of methoxy- and hydroxyl-substituted 2'-aminochalcones
Sulpizio, Chiara,Roller, Alexander,Giester, Gerald,Rompel, Annette
, p. 1747 - 1757 (2016)
Abstract: Three 2'-aminochalcone derivatives (E)-1-(2-aminophenyl)-3-(4-hydroxyphenyl)prop-2-en-1-one, (E)-1-(2-aminophenyl)-3-(3,4-dihydroxyphenyl)prop-2-en-1-one, and (E)-1-(2-amino-4,5-dimethoxyphenyl)-3-(4-methoxyphenyl)prop-2-en-1-one, have been synthesized, characterized, and tested in vitro in order to assess their antioxidant activity. All compounds were characterized on the basis of 1H NMR, 13C NMR, ESI-mass spectrometry, FT-IR, UV/Vis, and elemental analysis. The X-ray crystal structures of (E)-1-(2-aminophenyl)-3-(4-hydroxyphenyl)prop-2-en-1-one and (E)-1-(2-amino-4,5-dimethoxyphenyl)-3-(4-methoxyphenyl)prop-2-en-1-one were successfully determined showing a planar molecule geometry. Studies on the biological properties including test of free radical scavenging ability (DPPH test)?and superoxide dismutase mimetic activity were performed. The results indicate that the aminochalcone carrying two hydroxyl functionalities in adjacent meta and para position exhibits a stronger antioxidant activity than the other derivatives. Graphical abstract: [Figure not available: see fulltext.]
Hydroxy-substituted trans-cinnamoyl derivatives as multifunctional tools in the context of Alzheimer's disease
De Simone, Angela,Bartolini, Manuela,Baschieri, Andrea,Apperley, Kim Y.P.,Chen, Huan Huan,Guardigni, Melissa,Montanari, Serena,Kobrlova, Tereza,Soukup, Ondrej,Valgimigli, Luca,Andrisano, Vincenza,Keillor, Jeffrey W.,Basso, Manuela,Milelli, Andrea
, p. 378 - 389 (2017/08/21)
Alzheimer's disease (AD) is a multifactorial pathology that requires multifaceted agents able to address its peculiar nature. In recent years, a plethora of proteins and biochemical pathways has been proposed as possible targets to counteract neurotoxicity. Although the complex scenario is not completely elucidated, close relationships are emerging among some of these actors. In particular, increasing evidence has shown that aggregation of amyloid beta (Aβ), glycogen synthase kinase 3β (GSK-3β) and oxidative stress are strictly interconnected and their concomitant modulation may have a positive and synergic effect in contrasting AD-related impairments. We designed compound 3 which demonstrated the ability to inhibit both GSK-3β (IC50 = 24.36 ± 0.01 μM) and Aβ42 self-aggregation (IC50 = 9.0 ± 1.4 μM), to chelate copper (II) and to act as exceptionally strong radical scavenger (kinh = 6.8 ± 0.5 · 105 M?1s?1) even in phosphate buffer at pH 7.4 (kinh = 3.2 ± 0.5 · 105 M?1s?1). Importantly, compound 3 showed high-predicted blood-brain barrier permeability, did not exert any significant cytotoxic effects in immature cortical neurons up to 50 μM and showed neuroprotective properties at micromolar concentration against toxic insult induced by glutamate.
Inhibition of prostaglandin E2 production by synthetic minor prenylated chalcones and flavonoids: Synthesis, biological activity, crystal structure, and in silico evaluation
Rullah, Kamal,Mohd Aluwi, Mohd Fadhlizil Fasihi,Yamin, Bohari M.,Abdul Bahari, Mohd Nazri,Wei, Leong Sze,Ahmad, Syahida,Abas, Faridah,Ismail, Nor Hadiani,Jantan, Ibrahim,Wai, Lam Kok
supporting information, p. 3826 - 3834 (2014/09/16)
The discovery of potent inhibitors of prostaglandin E2 (PGE 2) synthesis in recent years has been proven to be an important game changer in pharmaceutical industry. It is known that excessive production of PGE2 triggers a
