16212-35-4Relevant academic research and scientific papers
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.
Discovery and characterization of novel CYP1B1 inhibitors based on heterocyclic chalcones: Overcoming cisplatin resistance in CYP1B1-overexpressing lines
Horley, Neill J.,Beresford, Kenneth J.M.,Chawla, Tarun,McCann, Glen J.P.,Ruparelia, Ketan C.,Gatchie, Linda,Sonawane, Vinay R.,Williams, Ibidapo S.,Tan, Hoon L.,Joshi, Prashant,Bharate, Sonali S.,Kumar, Vikas,Bharate, Sandip B.,Chaudhuri, Bhabatosh
, p. 159 - 174 (2017/02/23)
The structure of alpha-napthoflavone (ANF), a potent inhibitor of CYP1A1 and CYP1B1, mimics the structure of chalcones. Two potent CYP1B1 inhibitors 7k (DMU2105) and 6j (DMU2139) have been identified from two series of synthetic pyridylchalcones. They inh
Certain pyrazoline derivatives with kinase inhibitory activity
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Page/Page column 92, (2008/12/06)
The present invention provides certain pyrazoline compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions and methods of using the compositions in the treatment of various diseases.
