131231-24-8Relevant articles and documents
Selective Targeting of the TPX2 Site of Importin-α Using Fragment-Based Ligand Design
Holvey, Rhian S.,Valkov, Eugene,Neal, David,Stewart, Murray,Abell, Chris
, p. 1232 - 1239 (2015)
Protein-protein interactions are difficult therapeutic targets, and inhibiting pathologically relevant interactions without disrupting other essential ones presents an additional challenge. Herein we report how this might be achieved for the potential ant
2-(aryl (azacycloalkane-1-yl) methyl) phenol derivatives and uses thereof
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Paragraph 0371-0374; 0375-0377, (2021/07/24)
The invention discloses 2-(aryl (azacycloalkane-1-yl) methyl) phenol derivatives and application thereof, and belongs to the technical field of medicines. The invention provides a compound shown in a formula I or pharmaceutically acceptable salt thereof. The series of compounds have good inhibitory activity on the histone demethylase KDM4 family in vitro, the median inhibitory concentration (IC50) of most molecules on KDM4D is less than 500 nM, and the compounds have good inhibitory effect on proliferation of various human tumor cell strains in vitro, so that the series of compounds provide a new effective choice for developing targeted histone demethylase KDM4D drugs and preparing drugs for treating and/or preventing cancers and reproductive system diseases, and have good application prospects.
Iron(II)-Based Metalloradical Activation: Switch from Traditional Click Chemistry to Denitrogenative Annulation
Roy, Satyajit,Khatua, Hillol,Das, Sandip Kumar,Chattopadhyay, Buddhadeb
supporting information, p. 11439 - 11443 (2019/07/17)
A unique concept for the intermolecular denitrogenative annulation of 1,2,3,4-tetrazoles and alkynes was discovered by using a catalytic amount of Fe(TPP)Cl and Zn dust. The reaction precludes the traditional, more favored click reaction between an organic azide and alkynes, and instead proceeds by an unprecedented metalloradical activation. The method is anticipated to advance access to the construction of important basic nitrogen heterocycles, which will in turn enable discoveries of new drug candidates.
AMYLOID PROTEIN-SELECTIVE BACE INHIBITORS (ASBIS) FOR ALZHEIMER'S DISEASE
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Page/Page column 38; 39, (2019/09/18)
The present disclosure provides various compounds, compositions, and methods of BACE inhibition that interact with both BACE and APP to increase selectivity of the inhibitor. Compounds presented herein exhibit desirably low IC50 values and permeability ac
Synthesis and characterization of Sant-75 derivatives as Hedgehog-pathway inhibitors
Che, Chao,Li, Song,Yang, Bo,Xin, Shengchang,Yu, Zhixiong,Shao, Taofeng,Tao, Chuanye,Lin, Shuo,Yang, Zhen
scheme or table, p. 841 - 849 (2012/07/28)
Sant-75 is a newly identified potent inhibitor of the hedgehog pathway. We designed a diversity-oriented synthesis program, and synthesized a series of Sant-75 analogues, which lays the foundation for further investigation of the structure-activity relationship of this important class of hedgehog-pathway inhibitors.
[Pd(Cl)2(P(NC5H10)(C6H 11)2)2] - A highly effective and extremely versatile palladium-based negishi catalyst that efficiently and reliably operates at low catalyst loadings
Bolliger, Jeanne L.,Frech, Christian M.
experimental part, p. 11072 - 11081 (2010/11/16)
[Pd(Cl)2(P(NC5H10)-(C6H 11)2]2] (1) has been prepared in quantitative yield by reacting commercially available [Pd(cod)(Cl)2] (cod = cyclooctadiene) with readily prepared 1-(dicyclohexylphosphanyl)piperidine in toluene under N2 within a few minutes at room temperature. Complex 1 has proved to be an excellent Negishi catalyst, capable of quantitatively coupling a wide variety of electronically activated, non-activated, deactivated, sterically hindered, heterocyclic, and functionalized aryl bromides with various (also heterocyclic) arylzinc reagents, typically within a few minutes at 100°C in the presence of just 0.01 mol% of catalyst. Aryl bromides containing nitro, nitrile, ether, ester, hydroxy, carbonyl, and carboxyl groups, as well as acetais, lactones, amides, anilines, alkenes, carboxylic acids, acetic acids, and pyridines and pyrimidines, have been successfully used as coupling partners. Furthermore, electronic and steric variations are tolerated in both reaction partners. Experimental observations strongly indicate that a molecular mechanism is operative.
Palladium/tetraphosphine catalyzed suzuki cross-coupling of heteroarylboronic acids with aryl halides
Kondolff, Isabelle,Doucet, Henri,Santelli, Maurice
, p. 109 - 118 (2008/09/18)
(Chemical Equation Presented) cis,cis,cis-1,2,3,4- Tetrakis(diphenylphosphinomethyl)cyclopentane/[PdCl(C3H 5)]2 efficiently catalyses the Suzuki reaction of heteroarylboronic acids with aryl bromides and also the coupling of arylboronic acids with heteroaryl bromides. The coupling of thiophene- or benzothiopheneboronic acids, furan- or benzofuranboronic acids and 3-pyridineboronic acid with a variety of aryl bromides gave the corresponding coupling products in good yields. However, in most cases, better results in terms of ratio substrate/catalyst were obtained for the reverse reaction using heteroaryl bromides with arylboronic acids.
Suzuki coupling reactions of heteroarylboronic acids with aryl halides and arylboronic acids with heteroaryl bromides using a tetraphosphine/palladium catalyst
Kondolff, Isabelle,Doucet, Henri,Santelli, Maurice
, p. 2057 - 2061 (2007/10/03)
cix,cis,cis-1,2,3,4-Tetrakis(diphenylphosphinomethyl)cyclopentane/ [PdCl(C3H5)]2 efficiently catalyses the Suzuki reaction of heteroarylboronic acids with aryl bromides and also the coupling of arylboronic acids with heteroaryl bromides. The coupling of thiopheneboronic acids, 3-furanboronic acid and 3-pyridineboronic acid with a variety of aryl bromides gave the corresponding adducts in good yields. However, in most cases, better results in terms of substrate/catalyst ratio were obtained for the reaction of heteroaryl bromides with arylboronic acids. Georg Thieme Verlag Stuttgart.
Synthesis of novel palladacycles and their application in heck and Suzuki reactions under aerobic conditions
Xiong, Zhengchang,Wang, Nengdong,Dai, Mingji,Li, Ang,Chen, Jiahua,Yang, Zhen
, p. 3337 - 3340 (2007/10/03)
(Chemical Equation Presented) Design and synthesis of a novel family of furancarbothioamide-based palladacycles are reported herein. These palladacycles are thermally stable, not sensitive to air or moisture, and are applied effectively in the Heck reaction of aryl halides with terminal olefins and in the Suzuki reaction of aryl halides with arylboronic acids. These reactions were performed under aerobic conditions, leading to turnover numbers (TONs) up to 1 × 105.
Triazolo-pyridazine derivatives as ligands for GABA receptors
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, (2008/06/13)
1,2,4-triazolo[4,3-b]pyridazine derivatives, represented by wherein Z represents cyclobutyl, 1-methylcyclopentyl or pyrrolidin-1-yl, are selective ligands for GABAAreceptors, in particular having high affinity for the α2 and/or α3 subunit there
