- Enhanced cytotoxicity by a benzothiazole-containing cisplatin derivative in breast cancer cells
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In recent years, the concept of nanoparticles being used as an intelligent drug carrier has gained great attention. In this paper, the formulation of a liposome delivery system loaded with a novel benzothiazole-containing cisplatin derivative (CJM-Pt) was carried out. The particle size distributions were determined using dynamic light scattering, and the prepared liposomes showed a suitable size of around 98 nm. Stability studies showed that the CJM-Pt loaded liposomes were stable at 4 °C for more than four weeks. Investigation of triggered release indicated that the release performance of the prepared liposomes was controllable and the releasing effect was remarkable under low pH (42 °C). To test the suitability of the chosen formulation, CJM-Pt loaded liposomes were investigated against several tumor cell lines: MGC-803, SGC-7901, MCF-7 and MDA-MB-231. Furthermore, the cell cycle arrest was examined. The CJM-Pt loaded liposomes have the potential to be applied in drug delivery systems (DDS) for breast cancer therapy.
- You, Chaoqun,Yu, Jia,Sun, Yu,Luo, Yanghui,Zhang, Xiangyang,Zhu, Jin,Sun, Baiwang
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Read Online
- Aluminum Metal-Organic Framework-Ligated Single-Site Nickel(II)-Hydride for Heterogeneous Chemoselective Catalysis
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The development of chemoselective and heterogeneous earth-abundant metal catalysts is essential for environmentally friendly chemical synthesis. We report a highly efficient, chemoselective, and reusable single-site nickel(II) hydride catalyst based on robust and porous aluminum metal-organic frameworks (MOFs) (DUT-5) for hydrogenation of nitro and nitrile compounds to the corresponding amines and hydrogenolysis of aryl ethers under mild conditions. The nickel-hydride catalyst was prepared by the metalation of aluminum hydroxide secondary building units (SBUs) of DUT-5 having the formula of Al(μ2-OH)(bpdc) (bpdc = 4,4′-biphenyldicarboxylate) with NiBr2 followed by a reaction with NaEt3BH. DUT-5-NiH has a broad substrate scope with excellent functional group tolerance in the hydrogenation of aromatic and aliphatic nitro and nitrile compounds under 1 bar H2 and could be recycled and reused at least 10 times. By changing the reaction conditions of the hydrogenation of nitriles, symmetric or unsymmetric secondary amines were also afforded selectively. The experimental and computational studies suggested reversible nitrile coordination to nickel followed by 1,2-insertion of coordinated nitrile into the nickel-hydride bond occurring in the turnover-limiting step. In addition, DUT-5-NiH is also an active catalyst for chemoselective hydrogenolysis of carbon-oxygen bonds in aryl ethers to afford hydrocarbons under atmospheric hydrogen in the absence of any base, which is important for the generation of fuels from biomass. This work highlights the potential of MOF-based single-site earth-abundant metal catalysts for practical and eco-friendly production of chemical feedstocks and biofuels.
- Antil, Neha,Kumar, Ajay,Akhtar, Naved,Newar, Rajashree,Begum, Wahida,Dwivedi, Ashutosh,Manna, Kuntal
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p. 3943 - 3957
(2021/04/12)
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- SINGLE-STEP SYNTHESIS METHOD OF ARYL THIOL AND APPLICATION THEREOF
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The present invention relates to a single-step synthesis method of aryl thiol, and more specifically, to a method of synthesizing aryl thiol in a single-step by making aryl halide react with alkane dithiol in the presence of a transition metal catalyst. According to the present invention, a single-step synthesis method using the transition metal catalyst, the synthesis method which is capable of synthesizing aryl thiol from aryl halide at a high yield, can be provided. Various aryl halides may be applied to the synthesis method. Further, the synthesis method has advantages that an easily usable reagent may be used, operations are simple, and reactions can be performed under mild conditions. In addition, the synthesized aryl thiol may be used in the synthesis of advanced molecules such as diaryl sulfides and benzothiophenes.COPYRIGHT KIPO 2017
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Paragraph 0036; 0037; 0083; 0087; 0088; 0091
(2017/09/02)
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- Catalytic hydrogenation of sulfur-containing nitrobenzene over Pd/C catalysts: In situ sulfidation of Pd/C for the preparation of PdxSy catalysts
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The preparation of supported palladium sulfides catalysts has attracted much attention due to their good sulfur-resistant properties in the hydrogenation of sulfur-containing compounds. In this work, we unambiguously demonstrated that Pd/C catalyst could be in situ sulfided by organic sulfur-containing reactant molecules and the sulfidation was highly dependent on temperature. The in situ sulfidation of Pd/C catalyst was composed of a reaction of Pd with the sulfur derived from the cleavage of C-S bond of sulfur-containing reactant molecules, followed by a transformation to PdxSy at high temperatures (around 120 °C). The sulfided Pd/C catalyst could be used for at least 18 recycles without a significant loss in its activity during the hydrogenation of sulfur-containing nitrobenzene at 180 °C with 3 MPa H2, which could be attributed to the stable presence of Pd4S and Pd16S7.
- Zhang, Qunfeng,Xu, Wei,Li, Xiaonian,Jiang, Dahao,Xiang, Yizhi,Wang, Jianguo,Cen, Jie,Romano, Stephen,Ni, Jun
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- Hydrogen bond networks in five- and eight-membered palladium and platinum complexes derived from bis(2-aminophenyl)ether and bis(2-aminophenyl)thioether ligands
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The reaction of [MII(MeCN)2Cl2] (M = Pd, Pt) with the diamino ligands either bis(2-aminophenyl)ether or bis(2-aminophenyl)thioether {(NH2-C6H4)2D} [D = O (L1); D = S (L2)] yielded neutral coordination complexes of general formulae [M(Ln)Cl2] [M = Pd, n = 1 (1); Pt, n = 1 (2); Pd, n = 2 (3); Pd, n = 2 (4); Pt, n = 2 (5). The reaction of L2 with K2[PtCl6] promoted the mono-deprotonation of the diamino ligand to yield the neutral complex [PtIV{(NH2-C6H4)S(NH-C6H4)}Cl3] (6); when the H2[PtCl6] acid was used an ionic complex [PtIV(L2)Cl3]Cl (7) was obtained. All complexes were characterized by NMR in solution, vibrational spectroscopy, and by X-ray diffraction studies. The molecular structures of the complexes revealed different coordination patterns of the diamino ligands; L1 just displayed a κ2N mode meanwhile L2 exhibited a wide variety of patterns (κ2N, κNκS, and κ2NκS) forming chelate rings of five- or eight-members. The presence of N-H functions in the ligand moieties enhanced the formation of extended hydrogen-bond networks; these supramolecular arrangements were mainly discussed at unitary and binary levels and sorted according to the molecular coordination patterns observed.
- Hernández-Balderas, Uvaldo,Andrade-López, Noemí,Alvarado-Rodríguez, José G.,Moreno-Esparza, Rafael,Paneque, Margarita
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p. 165 - 174
(2015/04/27)
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- Unprecedented iminobenzosemiquinone and iminobenzoquinone coordinated mononuclear Cu(ii) complex formation under air
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Two non-innocent 2-anilino-4,6-di-tert-butylphenol units were connected through an -ortho bridging S atom and provided the ligand H4LS(AP/AP). The ligand reacted with CuCl2·2H2O in the presence of Et3
- Mondal, Manas Kumar,Biswas, Abul Kalam,Ganguly, Bishwajit,Mukherjee, Chandan
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p. 9375 - 9381
(2015/06/16)
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- Copper(II)-Catalyzed Single-Step Synthesis of Aryl Thiols from Aryl Halides and 1,2-Ethanedithiol
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A highly efficient transition metal-catalyzed single-step synthesis of aryl thiols from aryl halides has been developed employing copper(II) catalyst and 1,2-ethanedithiol. The key features are use of readily available reagents, a simple operation, and relatively mild reaction conditions. This new protocol shows a broad substrate scope with excellent functional group compatibility. A variety of aryl thiols are directly prepared from aryl halides in high yields. Furthermore, the aryl thiols are used in situ for the synthesis of more advanced molecules such as diaryl sulfides and benzothiophenes.
- Liu, Yajun,Kim, Jihye,Seo, Heesun,Park, Sunghyouk,Chae, Junghyun
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supporting information
p. 2205 - 2212
(2015/07/27)
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- Nanoscale Fe2O3-based catalysts for selective hydrogenation of nitroarenes to anilines
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Production of anilines - key intermediates for the fine chemical, agrochemical, and pharmaceutical industries - relies on precious metal catalysts that selectively hydrogenate aryl nitro groups in the presence of other easily reducible functionalities. Herein, we report convenient and stable iron oxide (Fe2O3) - based catalysts as a more earth-abundant alternative for this transformation. Pyrolysis of iron-phenanthroline complexes on carbon furnishes a unique structure in which the active Fe2O 3 particles are surrounded by a nitrogen-doped carbon layer. Highly selective hydrogenation of numerous structurally diverse nitroarenes (more than 80 examples) proceeded in good to excellent yield under industrially viable conditions.
- Jagadeesh, Rajenahally V.,Surkus, Annette-Enrica,Junge, Henrik,Pohl, Marga-Martina,Radnik, Joerg,Rabeah, Jabor,Huan, Heming,Schunemann, Volker,Brueckner, Angelika,Beller, Matthias
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p. 1073 - 1076
(2014/01/06)
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- Synthesis of new aza macrocyclic diamides 2,2'-diaminodiphenyl sulfide using crab-like method
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Six new aza crown ethers (4-9) were synthesized based on the conventional route crab-like method with the reaction of corresponding bis-α- chloroacetamidediphenylsulfide (BCADPS) (3) and aliphathic diamines (a-e) in refluxing acetonitrile in good yields.
- Shockravi, Abbas,Kamali, Mahmood
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scheme or table
p. 499 - 503
(2012/09/07)
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- Palladium-catalyzed C-S coupling: Access to thioethers, benzo[b]thiophenes, and thieno[3,2-b]thiophenes
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The first C-S bond formation/cross-coupling/cyclization domino reaction using thiourea as a cheap and easy to handle dihydrosulfide surrogate has been developed. Structurally important biarylthioether, benzo[b]thiophenes, and thieno[3,2-b]thiophene scaffolds are provided in high yield.
- Kuhn, Marius,Falk, Florian C.,Paradies, Jan
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supporting information; experimental part
p. 4100 - 4103
(2011/10/08)
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- Ligand-free copper-catalyzed synthesis of diaryl thioethers from aryl halides and thioacetamide
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Diaryl thioethers can be prepared via a copper-catalyzed cross-coupling between aryl halides and thioacetamide using Cs2CO3 as a base and DMSO-H2O as a solvent at 120 °C. Georg Thieme Verlag Stuttgart - New York.
- Tao, Chuanzhou,Lv, Aifeng,Zhao, Nan,Yang, Shuai,Liu, Xiaolang,Zhou, Jian,Liu, Weiwei,Zhao, Jing
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supporting information; experimental part
p. 134 - 138
(2011/03/22)
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- An imido-transfer reaction of aldehydes with N-sulfinylamines using vanadium and molybdenum oxochlorides as catalysts
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Vanadium and molybdenum oxochlorides were found to be efficient catalysts for imido-transfer between aldehydes and N-sulfinylamines.
- Zhizhin, Anton A.,Zarubin, Dmitry N.,Ustynyuk, Nikolai A.
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p. 699 - 702
(2008/09/17)
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- New potent inhibitors of trypanothione reductase from Trypanosoma cruzi in the 2-aminodiphenylsulfide series
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From a screening assay, 2-aminodiphenylsulfides were selected as leads for trypanothione reductase (TR) inhibition and studied by molecular modelling in the catalytic site of the enzyme. A series of analogues, monomers or bis-derivatives, were synthesized to improve binding energy and therefore inhibiting potency. These compounds appeared to be mixed competitive TR inhibitors and their inhibition profile could be explained when their aggregation in solution was taken into consideration. A bis-aminodiphenylsulfide with an IC50 of 0.55 μM was revealed to be the best TR inhibitor described so far.
- Girault,Baillet,Horvath,Lucas,Davioud-Charvet,Tartar,Sergheraert
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- Utilisations synthetiques d'une electrode soluble au soufre. IV. Creation de l'enchainement C-S-C a partir d'hydrocarbures aromatiques, d'heterocycles et d'amines aromatiques
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Use of a sacrificial sulfur electrode in electroorganic chemistry.IV.Formation of the C-S-C bond from aromatic hydrocarbons, heterocycles and aromatic amines.The electrophile S2+ was prepared in organic media by oxidation of a carbon-sulfur electrode.This species can react with aromatic hydrocarbons, heterocycles and aromatic amines to produce organic monosulfides. carbon-sulfur electrode / sacrificial electrode / sulfur cation / organic sulfide / electrophilic substitution
- Do, Quang Tho,Elothmani, Driss,Simonet, Jacques,Guillanton, Georges Le
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p. 789 - 793
(2007/10/02)
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