55532-22-4Relevant academic research and scientific papers
Discovery of styrylaniline derivatives as novel alpha-synuclein aggregates ligands
Bian, Jiang,Liu, Yi-Qi,He, Jie,Lin, Xin,Qiu, Chen-Yang,Yu, Wen-Bo,Shen, Yan,Zhu, Ze-Yun,Ye, De-Yong,Wang, Jian,Chu, Yong
, (2021/10/06)
Parkinson's disease (PD) is the second most common neurodegenerative disorder. Early diagnosis is the key to treatment but is still a great challenge in the clinic now. The discovery of alpha-synuclein (α-syn) aggregates ligands has become an attractive s
Activation of anti-oxidant Nrf2 signaling by substituted trans stilbenes
Deck, Lorraine M.,Whalen, Lisa J.,Hunsaker, Lucy A.,Royer, Robert E.,Vander Jagt, David L.
, p. 1423 - 1430 (2017/02/18)
Nrf2, which is a member of the cap'n’ collar family of transcription factors, is a major regulator of phase II detoxification and anti-oxidant genes as well as anti-inflammatory and neuroprotective genes. The importance of inflammation and oxidative stress in many chronic diseases supports the concept that activation of anti-oxidant Nrf2 signaling may have therapeutic potential. A number of Nrf2 activators have entered into clinical trials. Nrf2 exists in the cytosol in complex with its binding partner Keap1, which is a thiol-rich redox-sensing protein. In response to oxidative and electrophilic stress, select cysteine residues of Keap1 are modified, which locks Keap1 in the Nrf2-Keap1 complex and allows newly synthesized Nrf2 to enter the nucleus. Numerous Nrf2-activating chemicals, including a number of natural products, are electrophiles that modify Keap1, often by Michael addition, leading to activation of Nrf2. One concern with the design of Nrf2 activators that are electrophilic covalent modifiers of Keap1 is the issue of selectivity. In the present study, substituted trans stilbenes were identified as activators of Nrf2. These activators of Nrf2 are not highly electrophilic and therefore are unlikely to activate Nrf2 through covalent modification of Keap1. Dose-response studies demonstrated that a range of substituents on either ring of the trans stilbenes, especially fluorine and methoxy substituents, influenced not only the sensitivity to activation, reflected in EC50values, but also the extent of activation, which suggests that multiple mechanisms are involved in the activation of Nrf2. The stilbene backbone appears to be a privileged scaffold for development of a new class of Nrf2 activators.
Synthesis and bioactivity of resveratrol analogues
Ao, Junli,Chen, Yuanmou,Xu, Xiaoling,Zhang, Xu,Yu, Yue,Yu, Peng,Hua, Erbing
, p. 2092 - 2098 (2014/06/09)
It has been reported that resveratrol enhanced SIRT1 expression and significantly mimicked calorie restriction by stimulating Sir2 which is the most homologic homologue of SIRT1 of mammalian. A series of novel resveratrol derivatives were designed and synthesized as novel SIRT1 activator candidates. These synthesized compounds were characterized by spectral (1H NMR) analysis and examined for their Sir2 activation against yeast parental strain-BY4743 at a concentration of 100 μM/L by Bioscreen C MBR machine. Several compounds showed a promising Sir2 activation activity compared with resveratrol. Meanwhile, the structure-activity relationships with Sirt2 activation activities were also discussed.
Compounds for use as therapeutic agents affecting p53 expression and/or activity
-
Page/Page column 46, (2012/10/18)
The present invention relates to compound (I) wherein R1 and R2 independently represent a hydrogen atom, a (C1-C4)alkoxy group, a fluoro(C1-C4)alkoxy group, a hydroxyl group, a benzyloxy group, a di(C1-C4)alkylamino group, a pyridyl-vinyl group, a pyrimidinyl-vinyl group, a styryl group, or a -NHCOphenyl group; R3, R4 and R5 independently represent a hydrogen atom, a (C1-C4)alkyl group, a CONHR6 group, a -CONR7R8 group, a -SO2NHR6 group, or a heteroaryl group optionally substituted by a halogen atom, a -(CH2)nNR7R8 group or a hydroxy(C1-C4)alkyl group; R6 represents a hydrogen atom, a -(CHR9)m(CH2)nNR7R8 group or a (C1-C6)alkyl group optionally substituted by a hydroxyl group; or anyone of its pharmaceutically acceptable salt, for use as an agent for preventing, inhibiting or treating a disease in a patient suffering thereof, said disease involving a deregulated p53. Some of said compounds are new and also form part of the invention.
Microwave-assisted wittig reaction of semistabilized nitro-substituted benzyltriphenyl-phosphorous ylides with aldehydes in phase-transfer conditions
Rodrigues, Tiago,Lopes, Francisca,Moreira, Rui
experimental part, p. 747 - 755 (2011/12/15)
We report here a simple entry into the nitrostilbene system in very short reaction times and good yields using the microwave-assisted Wittig reaction in phase-transfer conditions of nitro-substituted benzyltriphenylphosphonium ylides with aldehydes. Taylor & Francis Group, LLC.
Palladium-catalyzed decarboxylative cross-coupling reaction of cinnamic acid with aryl iodide
Wang, Zhiyong,Ding, Qiuping,He, Xiaodan,Wu, Jie
supporting information; experimental part, p. 863 - 865 (2009/05/30)
A highly effective decarboxylative cross-coupling reaction of cinnamic acid with aryl iodide catalyzed by the combination of palladium chloride and CyJohnPhos in the presence of Ag2CO3 as an additive is described. The desired carbon-
Separation of α-glucosidase-inhibitory and liver X receptor-antagonistic activities of phenethylphenyl phthalimide analogs and generation of LXRα-selective antagonists
Motoshima, Kazunori,Noguchi-Yachide, Tomomi,Sugita, Kazuyuki,Hashimoto, Yuichi,Ishikawa, Minoru
experimental part, p. 5001 - 5014 (2009/12/24)
Liver X receptor (LXR) α/β dual agonists are candidate medicaments for the treatment of metabolic syndrome, because their biological actions include increasing cholesterol efflux mediated by LXRβ. However, their clinical application is currently limited by their enhancing effect on triglyceride (TG) synthesis mediated by LXRα. Combination of an LXRα-selective antagonist with an LXRα/β dual agonist may overcome this disadvantage. In the present work, structural development studies of phenethylphenyl phthalimide 9, which possesses LXRα/β dual-antagonistic activity and α-glucosidase-inhibitory activity, led to the LXRα-selective antagonist 23f. Specific α-glucosidase inhibitors were also obtained.
