1253-46-9Relevant articles and documents
Balancing Mechanical Stability and Ultrahigh Porosity in Crystalline Framework Materials
H?nicke, Ines M.,Senkovska, Irena,Bon, Volodymyr,Baburin, Igor A.,B?nisch, Nadine,Raschke, Silvia,Evans, Jack D.,Kaskel, Stefan
, p. 13780 - 13783 (2018)
A new mesoporous metal–organic framework (MOF; DUT-60) was conceptually designed in silico using Zn4O6+ nodes, ditopic and tritopic linkers to explore the stability limits of framework architectures with ultrahigh porosity. The robus
Structure of aggregates of trans-4-alkoxy-4′-carboxystilbenes in the solid state and in microheterogeneous media. A link between the `unit aggregate' and extended arrays
Vaday,Geiger,Cleary,Perlstein,Whitten
, p. 321 - 329 (1997)
Crystals of three 4-alkoxy-4′-carboxy trans-stilbene (ACS) derivatives and a crystal of 4-methoxy-4′-methanoate trans-stilbene have been shown to have structures in which the amphiphilic aromatics are arranged in layers remarkably similar to deposited Langmuir-Blodgett multilayer assemblies. Within each layer there is either a glide or pseudoglide (or herringbone) arrangement of the chromophores very similar to that deduced from physical properties and simulations for structurally related stilbene, azobenzene, and tolan amphiphiles in microheterogeneous media, solution, and Langmuir-Blodgett (LB) films. The fluorescence of the crystals is very similar to that associated with LB films of a water-insoluble amphiphilic ACS that is associated with the aggregate. An analysis of the crystal structure indicates that energetically favorable aromatic-aromatic (edge-face) interaction determines the packing within a layer.
Vinyl-Stilbene Compounds and Uses Thereof
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Paragraph 0255; 0288-0294, (2021/06/22)
The present invention relates to a biphenyl - stilbene (Vinyl-stilbene) - based compound and a pharmaceutical composition for preventing or treating norovirus infection comprising the same as an active ingredient. The present invention can be usefully used as a pharmaceutical composition for treating norovirus infection by showing superior norovirus inhibitory activity and lower cell toxicity as compared to previously known compounds.
Reactions of benzyltriphenylphosphonium salts under photoredox catalysis
Boldt, Andrew M.,Dickinson, Sidney I.,Ramirez, Jonathan R.,Benz-Weeden, Anna M.,Wilson, David S.,Stevenson, Susan M.
supporting information, p. 7810 - 7815 (2021/09/28)
The development of benzyltriphenylphosphonium salts as alkyl radical precursors using photoredox catalysis is described. Depending on substituents, the benzylic radicals may couple to form C-C bonds or abstract a hydrogen atom to form C-H bonds. A natural product, brittonin A, was also synthesized using this method.
Anti-oligomerization sheet molecules: Design, synthesis and evaluation of inhibitory activities against α-synuclein aggregation
Liu, Hao,Chen, Li,Zhou, Fei,Zhang, Yun-Xiao,Xu, Ji,Xu, Meng,Bai, Su-Ping
supporting information, p. 3089 - 3096 (2019/06/14)
Aggregation of α-synuclein (α-Syn) play a key role in the development of Parkinson Disease (PD). One of the effective approaches is to stabilize the native, monomeric protein with suitable molecule ligands. We have designed and synthesized a series of sheet-like conjugated compounds which possess different skeletons and various heteroatoms in the two blocks located at both ends of linker, which have good π-electron delocalization and high ability of hydrogen-bond formation. They have shown anti-aggregation activities in vitro towards α-Syn with IC50 down to 1.09 μM. The molecule is found binding in parallel to the NACore within NAC domain of α-Syn, interfering aggregation of NAC region within different α-Syn monomer, and further inhibiting or slowing down the formation of α-Syn oligomer nuclei at lag phase. The potential inhibitor obtained by our strategy is considered to be highly efficient to inhibit α-Syn aggregation.
Identification of novel non-nucleoside vinyl-stilbene analogs as potent norovirus replication inhibitors with a potential host-targeting mechanism
Harmalkar, Dipesh S.,Lee, Sung-Jin,Lu, Qili,Kim, Mi Il,Park, Jaehyung,Lee, Hwayoung,Park, Minkyung,Lee, Ahrim,Lee, Choongho,Lee, Kyeong
supporting information, (2019/10/09)
Norovirus (NV), is the most common cause of acute gastroenteritis worldwide. To date, there is no specific anti-NV drug or vaccine to treat NV infections. In this study, we evaluated the inhibitory effect of different stilbene-based analogs on RNA genome replication of human NV (HNV) using a virus replicon-bearing cell line (HG23). Initial screening of our in-house chemical library against NV led to the identification of a hit containing stilbene scaffold 5 which on initial optimization gave us a vinyl stilbene compound 16c (EC50 = 4.4 μM). Herein we report our structure-activity relationship study of the novel series of vinyl stilbene analogs that inhibits viral RNA genome replication in a human NV-specific manner. Among these newly synthesized compounds, several amide derivatives of vinyl stilbenes exhibited potent anti-NV activity with EC50 values ranging from 1 to 2 μM. A trans-vinyl stilbenoid with an appended substituted piperazine amide (18k), exhibited potent anti-NV activity and also displayed favorable metabolic stability. Compound 18k demonstrated an excellent safety profile, the highest suppressive effect, and was selective for HNV replication via a viral RNA polymerase-independent manner. Its potential host-targeting antiviral mechanism was further supported by specific activation of heat shock factor 1-dependent stress-inducible pathway by 18k. These results suggest that 18k might be a promising lead compound for developing novel NV inhibitors with the novel antiviral mechanism.
HISTONE DEACETYLASE INHIBITORS
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Paragraph 00256; 00257; 00266; 00267; 00276; 00277; 00318, (2018/07/29)
Provided herein are compounds and methods for inhibiting histone deacetylase ("HDAC") enzymes (e.g., HDAC1, HDAC2, and HDAC3).
ANTI-ESTROGENIC COMPOUNDS
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Page/Page column 0156-0159, (2016/11/14)
The present disclosure provides a compound of Formula I: or a pharmaceutically acceptable salt wherein X, R1-R8, Y1-Y5, m, n, p, and q are defined herein. The novel 2H-chromene compounds are useful for the modul
SUBSTITUTED BICYCLIC HETEROARYL COMPOUNDS AS RXR AGONISTS
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Paragraph 0428, (2016/12/01)
The present invention relates to certain substituted bicyclic compounds that are agonists of RXR and which are therefore useful in the treatment of certain disorders that can be prevented or treated by activation of this receptor. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders.
One-pot synthesis of gem-difluorostyrenes from benzyl bromide via olefination of phosphonium ylide with difluorocarbene
Deng, Xiao-Yun,Lin, Jin-Hong,Xiao, Ji-Chang
, p. 116 - 120 (2015/11/10)
A new approach for the synthesis of gem-difluorostyrenes from benzyl bromide is described. Quaternization of triphenylphosphine with benzyl bromide to give phosphonium salts, deprotonation of the corresponding phosphonium salts to produce phosphonium ylide, and the subsequent olefination of phosphonium ylide with difluorocarbene generated from difluoromethylene phosphobetaine (Ph3P+CF2CO2-) by decarboxylation can occur smoothly in one-pot, furnishing the final gem-difluorostyrenes in good yields.