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
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.
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
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
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.
Selective synthesis of mono- and di-methylated amines using methanol and sodium azide as C1 and N1 sources
Chakrabarti, Kaushik,Mishra, Anju,Panja, Dibyajyoti,Paul, Bhaskar,Kundu, Sabuj
supporting information, p. 3339 - 3345 (2018/07/29)
A Ru(ii) complex mediated synthesis of various N,N-dimethyl and N-monomethyl amines from organic azides using methanol as a methylating agent is reported. This methodology was successfully applied for a one-pot reaction of bromide derivatives and sodium azide in methanol. Notably, by controlling the reaction time several N-monomethylated and N,N-dimethylated amines were synthesized selectively. The practical applicability of this tandem process was revealed by preparative scale reactions with different organic azides and synthesis of an anti-vertigo drug betahistine. Several kinetic experiments and DFT studies were carried out to understand the mechanism of this transformation.
