25419-86-7Relevant academic research and scientific papers
Induction of apoptosis in Ehrlich ascites tumour cells via p53 activation by a novel small-molecule MDM2 inhibitor – LQFM030
da Mota, Mariana F.,Cortez, Alane P.,Benfica, Polyana L.,Rodrigues, Bruna dos S.,Castro, Thalyta F.,Macedo, Larissa M.,Castro, Carlos H.,Li?o, Luciano M.,de Carvalho, Flávio S.,Romeiro, Luiz A. S.,Menegatti, Ricardo,Verli, Hugo,Villavicencio, Bianca,Valadares, Marize C.
, p. 1143 - 1159 (2016)
Objective: The activation of the p53 pathway through the inhibition of MDM2 has been proposed as a novel therapeutic strategy against tumours. A series of cis-imidazoline analogues, termed nutlins, were reported to displace the recombinant p53 protein fro
Design, synthesis and pharmacological profile of novel dopamine D2 receptor ligands
Menegatti, Ricardo,Cunha, Anna C.,Ferreira, Vitor F.,Perreira, Edna F. R.,El-Nabawi, Ahmed,Eldefrawi, Amira T.,Albuquerque, Edson X.,Neves, Gilda,Rates, Stela M. K.,Fraga, Carlos A. M.,Barreiro, Eliezer J.
, p. 4807 - 4813 (2003)
The present study describes the synthesis and pharmacological profile of three novel heterocyclic compounds originally designed, on the basis of bioisosterism, as dopamine D2 receptor ligands: 1-[1-(4-chlorophenyl)-1H-pyrazol-4-ylmethyl]-4-phenyl-piperazi
The novel piperazine-containing compound LQFM018: Necroptosis cell death mechanisms, dopamine D4 receptor binding and toxicological assessment
Costa, Fabiana Bettanin,Cortez, Alane P.,de ávila, Renato Ivan,de Carvalho, Flávio S.,Andrade, Wanessa M.,da Cruz, Andrezza F.,Reis, Karinna B.,Menegatti, Ricardo,Li?o, Luciano M.,Romeiro, Luiz Ant?nio S.,No?l, Fran?ois,Fraga, Carlos Alberto M.,Barreiro, Eliezer J.,Sanz, Germán,Rodrigues, Marcella F.,Vaz, Boniek G.,Valadares, Marize Campos
, p. 481 - 493 (2018)
Piperazine is a promising scaffold for drug development due to its broad spectrum of biological activities. Based on this, the new piperazine-containing compound LQFM018 (2) [ethyl 4-((1-(4-chlorophenyl)-1H-pyrazol-4-yl)methyl)piperazine-1-carboxylate] wa
Copper pyrithione (CuPT)-catalyzed/mediated amination and thioarylation of (hetero)aryl halides: A competition
Cao, Ningtao,Song, Bao,Xie, Jianwei,Zhang, Jie
, (2021/11/08)
A facile method for the synthesis of N-arylheterocycles and di(hetero)aryl sulfides under mild condition is described. In these transformations, copper pyrithione (CuPT) was used as the copper catalyst for C─N coupling, while served as catalyst and coupled partner for C─S coupling with high yields and broad substrate tolerance. The S-arylation process was also utilized for the construction of valuable bioactive 2-sulfonylpyridine 1-oxide derivatives.
Organophotochemical SNAr Reactions of Mildly Electron-Poor Fluoroarenes
Burton, Jonathan W.,Genovino, Julien,Lian, Yajing,Monck, Nat,Sheridan, Thomas,Yayla, Hatice G.
supporting information, p. 2766 - 2770 (2020/05/18)
C–F functionalization of arenes with a range of alcohol and pyrazole nucleophiles has been achieved without the need for metal catalysts or highly electron-poor substrates. Treatment of fluoroarenes with alcohols or pyrazoles and DDQ under irradiation by blue LED light provides the corresponding substituted products. The procedure is complementary to classical SNAr chemistry which generally requires basic reaction conditions and high temperatures, and provides products under non-basic conditions at ≈ 40 °C.
Ruthenium-Catalyzed ortho- And meta-H/D Exchange of Arenes
Zhao, Liang-Liang,Liu, Wei,Zhang, Zengyu,Zhao, Hongyan,Wang, Qi,Yan, Xiaoyu
supporting information, p. 10023 - 10027 (2019/12/24)
Ruthenium-catalyzed aromatic H/D exchange in [D4]acetic acid has been developed. By using N-heteroarenes as directing groups, both ortho and meta positions are selectively deuterated with high levels of D incorporation. Moreover, this strategy provides an alternative way to achieve meta-C-H activation.
Efficient copper-catalyzed N-arylation of NH-containing heterocycles and sulfonamides with arenediazonium tetrafluoroborates
Ouyang, Yu-Qing,Yang, Zhen-Hua,Chen, Zhong-Hui,Zhao, Sheng-Yin
, p. 771 - 778 (2017/04/06)
A practical copper-catalyzed N-arylation of NH-containing heterocycles with arenediazonium tetrafluoroborates has been developed using CuCl as catalyst and K2CO3 as additive under ligand-free conditions. This reaction system has wide substrate scope including imides, 1H-pyrazole, 1H-tetrazoles, 1,2-benzisothiazol-3(2H)-one, and related sulfonamides and gives moderate to excellent yields (up to 95%) of the desired products. This strategy is very general, simple, environmentally friendly, and tolerant of oxygen.
PYRAZOLYL PYRIMIDINAMINE COMPOUND AND APPLICATION THEREOF
-
Paragraph 0366; 0367, (2016/12/01)
Disclosed are pyrazolyl pyrimidinamine compounds with structures as shown in Formula I: The definitions of each of the substituents can be seen in the description. The compounds of present invention have a broad spectrum of bactericidal, insecticidal and acaricidal activity, and have good control effect on downy mildew of cucumber, powdery mildew of wheat, corn rust, anthracnosis of cucumber and the like, and especially have better control effect on downy mildew of cucumber, powdery mildew of wheat and anthracnosis of cucumber. The compounds of present invention also show good insecticidal activity, part of the compounds, at very low doses, have excellent control effect on diseases caused by Plutella xylostella, armyworm, Myzus persicae, Tetranychus cinnabarinus etc.
Facile Synthesis of 1-Arylpyrazoles
Yang, Yiwen,Kuang, Chunxiang
supporting information, p. 2281 - 2284 (2015/08/03)
A convenient and transition-metal-free synthesis of 1-arylpyrazoles that involves the cycloaddition of 3-arylsydnones and acrylic acid is presented. The process proceeds smoothly to obtain the target products with moderate to high yields.
Aromatic N-arylations catalyzed by copper-anchored porous zinc-based metal-organic framework under heterogeneous conditions
Maity, Tanmoy,Saha, Debraj,Koner, Subratanath
, p. 2373 - 2383 (2014/08/18)
A highly porous Zn-based metal-organic framework (MOF) IRMOF-3 was covalently decorated with pyridine-2-aldehyde. The free amine group of IRMOF-3 upon condensation with pyridine-2-aldehyde affords a bidentate Schiff-base moiety in the porous matrix. The Schiff base moieties are availed to anchor copper(II) ions to display the catalyst's utility towards catalytic reactions. The catalyst was characterized by UV/Vis and IR spectroscopy, powder XRD spectrometry, SEM energy-dispersive X-ray spectrometry, and nitrogen sorption measurements. The catalyst exhibits excellent activity in catalyzing the N-arylation reaction of nitrogen-containing heterocycles with aryl bromides in DMSO medium, under mild condition (90°C) in the presence of Cs 2CO3. The porous catalyst demonstrates size selectivity towards substrate as a result of the presence of active sites inside the pores of the MOF. The anchored complex seems to be not leached or decomposed during the catalytic reactions up to five successive catalytic cycles, demonstrating practical advantages over homogeneous catalysis.
