94341-53-4Relevant academic research and scientific papers
Synthesis, Antimicrobial Activity, and Molecular Docking of Benzoic Hydrazide or Amide Derivatives Containing a 1,2,3-Triazole Group as Potential SDH Inhibitors
Ding, Yue,Zhang, Ling,Yang, Song,Li, Zhong,Wang, Pei-Yi
, p. 1319 - 1330 (2021)
The present study was carried out in an attempt to synthesize a new class of antimicrobial agents containing a 1,2,3-triazole motif formed by classical copper catalyzed click chemistry. Antifungal bioassay results showed that five compounds 5a, 5e, 5h, 5j
1, 2, 3-triazole hydrazide or amide compound as well as preparation method and application thereof
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Paragraph 0031; 0053-0054, (2021/04/03)
The invention relates to 1, 2, 3, -triazole hydrazide or amide compounds as well as a preparation method and application thereof. The compound has a structure as shown in a general formula (I) which is described in the specification. On the basis of methy
Inverted positioning of dnmt1 inhibitor in the active site of dnmt1 caused by hydrophobicity/hydrophilicity of the terminal structure
Kondo, Takeshi,Kubo, Yuhei,Tojo, Toshifumi,Yuasa, Makoto
, p. 2372 - 2378 (2021/12/16)
DNA (cytosine-5)-methyltransferase 1 (DNMT1) is one of the enzymes that regulate DNA modification. It has been demonstrated that overexpression of DNMT1 is associated with the development of cancer, making DNMT1 an attractive molecular target for cancer t
MTOR/HDAC dual inhibitor and application thereof
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Paragraph 0141-0144, (2020/11/12)
The invention discloses an mTOR/HDAC dual inhibitor and application thereof, and the dual inhibitor has dual inhibition effects of mTOR and HDAC, has better curative effect than the mTOR inhibitor, and can be used for preparing anti-tumor and anti-idiopat
Spiroindoline-Capped Selective HDAC6 Inhibitors: Design, Synthesis, Structural Analysis, and Biological Evaluation
Saraswati, A. Prasanth,Relitti, Nicola,Brindisi, Margherita,Osko, Jeremy D.,Chemi, Giulia,Federico, Stefano,Grillo, Alessandro,Brogi, Simone,McCabe, Niamh H.,Turkington, Richard C.,Ibrahim, Ola,O'Sullivan, Jeffrey,Lamponi, Stefania,Ghanim, Magda,Kelly, Vincent P.,Zisterer, Daniela,Amet, Rebecca,Hannon Barroeta, Patricia,Vanni, Francesca,Ulivieri, Cristina,Herp, Daniel,Sarno, Federica,Di Costanzo, Antonella,Saccoccia, Fulvio,Ruberti, Giovina,Jung, Manfred,Altucci, Lucia,Gemma, Sandra,Butini, Stefania,Christianson, David W.,Campiani, Giuseppe
supporting information, p. 2268 - 2276 (2020/12/17)
Histone deacetylase inhibitors (HDACi) have emerged as promising therapeutics for the treatment of neurodegeneration, cancer, and rare disorders. Herein, we report the development of a series of spiroindoline-based HDAC6 isoform-selective inhibitors based on the X-ray crystal studies of the hit 6a. We identified compound 6j as the most potent and selective hHDAC6 inhibitor of the series. Biological investigation of compounds 6b, 6h, and 6j demonstrated their antiproliferative activity against several cancer cell lines. Western blotting studies indicated that they were able to increase tubulin acetylation, without significant variation in histone acetylation state, and induced PARP cleavage indicating their apoptotic potential at the molecular level. 6j induced HDAC6-dependent pSTAT3 inhibition.
Screening of Three Transition Metal-Mediated Reactions Compatible with DNA-Encoded Chemical Libraries
Favalli, Nicholas,Bassi, Gabriele,Zanetti, Tania,Scheuermann, J?rg,Neri, Dario
, (2019/04/08)
The construction of DNA-encoded chemical libraries (DECLs) crucially relies on the availability of chemical reactions, which are DNA-compatible and which exhibit high conversion rates for a large number of diverse substrates. In this work, we present our
Naphthoquinone-fused triazole core skeleton derivative compound, preparation method and application thereof
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Paragraph 0043; 0053-0057; 0157-0161; 0248-0255, (2019/10/01)
The invention relates to a naphthoquinone-fused triazole core skeleton derivative compound, relates to a preparation method and application of the naphthoquinone-triazole core skeleton derivative compound, and belongs to the field of organic chemistry. Th
An efficient NaHSO3-promoted protocol for chemoselective synthesis of 2-substituted benzimidazoles in water
Jiang, Yu-Qin,Jia, Shu-Hong,Li, Xi-Yong,Sun, Ya-Min,Li, Wei,Zhang, Wei-Wei,Xu, Gui-Qing
, p. 1265 - 1276 (2019/01/28)
An efficient protocol for chemoselective synthesis of 2-substituted benzimidazoles from a variety of aliphatic/aromatic/ heteroaryl aldehydes and o-phenylenediamine derivatives promoted by NaHSO3 in water had been developed. The amount of NaHSO3 had a great effect on the reaction selectivity of 2-substituted benzimidazole and 1,2-disubstituted benzimidazole when the reaction was carried out in water. When the amount of the NaHSO3 was more than 11 equivalents, the 2-substituted benzimidazole could be highly selectively formed as the sole product. NaHSO3 was firstly reacted with aldehyde to form the aldehyde sodium bisulfite, which reacted with o-phenylenediamine to form the 2-substituted benzimidazole and inhibited the formation of 1,2-disubstituted benzimidazole. This protocol solved the poor selectivity problem appearing in traditional method when cyclocondensation between o-phenylenediamine and aldehydes. The method also had advantage of simple work up by filtrating the single 2-substituted benzimidazole precipitates from reaction mixture at the end of the reaction without further purification. In addition, the method was applicable to both electron-rich and electron-poor starting materials, which was successfully used for synthesizing nine novel 2-substituted benzimidazole derivatives containing a 1,2,3-triazole moiety. They were characterized by NMR, IR and HRMS spectrum. Moreover, this method had been applied to a large scale synthesis of 2-substituted benzimidazole derivatives.
Transient Protection of Organic Azides from Click Reactions with Alkynes by Phosphazide Formation
Meguro, Tomohiro,Yoshida, Suguru,Igawa, Kazunobu,Tomooka, Katsuhiko,Hosoya, Takamitsu
supporting information, p. 4126 - 4130 (2018/07/15)
A method for protecting organic azides from click reactions with alkynes is reported. Treatment of azides with Amphos affords phosphazides, which are stable under click reaction conditions and are easily converted back to azides by treatment with elemental sulfur. Thus, the method allows for facile modification of azide compounds via site-selective click reactions.
Sustainable organophosphorus-catalysed Staudinger reduction
Lenstra, Danny C.,Lenting, Peter E.,Mecinovi?, Jasmin
supporting information, p. 4418 - 4422 (2018/10/17)
A highly efficient and sustainable catalytic Staudinger reduction for the conversion of organic azides to amines in excellent yields has been developed. The reaction displays excellent functional group tolerance to functionalities that are otherwise prone to reduction, such as sulfones, esters, amides, ketones, nitriles, alkenes, and benzyl ethers. The green nature of the reaction is exemplified by the use of PMHS, CPME, and a lack of column chromatography.
