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Keywords = N-hydroxyphthalimide

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21 pages, 6387 KiB  
Article
Carbon Dot-Enhanced Doxorubicin Liposomes: A Dual-Functional Nanoplatform for Cancer Therapy
by Corina-Lenuta Logigan, Cristian Peptu, Corneliu S. Stan, Gabriel Luta, Crina Elena Tiron, Mariana Pinteala, Aleksander Foryś, Bogdan Simionescu, Constanta Ibanescu, Adrian Tiron and Catalina A. Peptu
Int. J. Mol. Sci. 2025, 26(15), 7535; https://doi.org/10.3390/ijms26157535 - 4 Aug 2025
Abstract
Liposomes (LPs) represent one of the most effective nanoscale platforms for drug delivery in cancer therapy due to their favorable pharmacokinetic and various body tissue compatibility profiles. Building on recent findings showing that carbon dots derived from N-hydroxyphthalimide (CDs-NHF) possess intrinsic antitumor activity, [...] Read more.
Liposomes (LPs) represent one of the most effective nanoscale platforms for drug delivery in cancer therapy due to their favorable pharmacokinetic and various body tissue compatibility profiles. Building on recent findings showing that carbon dots derived from N-hydroxyphthalimide (CDs-NHF) possess intrinsic antitumor activity, herein, we investigate the possibility of preparing complex nano-platforms composed of LPs encapsulating CDs-NHF and/or doxorubicin (DOX) for breast and lung cancer. Various LP formulations were prepared and characterized using Cryo-TEM and Cryo-SEM for morphological analysis, while zeta potential and fluorescence assessments confirmed their stability and optical properties. Cellular effects were evaluated through immunofluorescence microscopy and proliferation assays. LPs-CDs-NHF significantly reduced cancer cell viability at lower concentrations compared to free CDs-NHF, and this effect was further amplified when combined with doxorubicin. Mechanistically, the liposomal formulations downregulated key signaling molecules including pAKT, pmTOR, and pERK, indicating the disruption of cancer-related pathways. These findings suggest that LPs containing CDs-NHF, either alone or in combination with DOX, exhibit synergistic antitumor activity and hold strong promise as multifunctional nanocarriers for future oncological applications. Full article
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11 pages, 1791 KiB  
Article
An Investigation of N-Hydroxyphthalimide Catalyzed Aerobic Oxidation of Toluene without Metal Ions in Liquid Phase: Effect of Solvents and Phase Transfer Catalysts
by Guojun Shi, Longsheng Dong and Ya Feng
Molecules 2024, 29(13), 3066; https://doi.org/10.3390/molecules29133066 - 27 Jun 2024
Cited by 2 | Viewed by 1339
Abstract
The selective oxidation of toluene to yield value-added oxygenates, such as benzyl alcohol, benzaldehyde, and benzoic acid, via dioxygen presents a chlorine-free approach under benign conditions. Metal-free catalytic processes are preferred to avoid metal ion contamination. In this study, we employed N-hydroxyphthalimide (NHPI) [...] Read more.
The selective oxidation of toluene to yield value-added oxygenates, such as benzyl alcohol, benzaldehyde, and benzoic acid, via dioxygen presents a chlorine-free approach under benign conditions. Metal-free catalytic processes are preferred to avoid metal ion contamination. In this study, we employed N-hydroxyphthalimide (NHPI) as a catalyst for the aerobic oxidation of toluene to its oxygenated derivatives. The choice of solvent exerted a significant impact on the catalytic activity and selectivity of the catalyst NHPI at reaction temperatures exceeding 70 °C. Notably, hexafluoroisopropanol substantially enhanced the selective production of benzaldehyde. Furthermore, we identified didecyl dimethyl ammonium bromide, featuring two symmetrical long hydrophobic chains, as a potent enhancer of NHPI for the solvent-free aerobic oxidation of toluene. This effect is ascribed to its unique symmetrical structure, extraction capabilities, and resistance to thermal and acid/base conditions. Based on the product distribution and control experiments, we proposed a plausible reaction mechanism. These findings may inform the industrial synthesis of oxygenated derivatives from toluene. Full article
(This article belongs to the Section Physical Chemistry)
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10 pages, 764 KiB  
Article
Efficient Synthesis of 2-Ethylhexanoic Acid via N-Hydroxyphthalimide Catalyzed Oxidation of 2-Ethylhexanal with Oxygen
by Łukasz Czieszowic, Beata Orlińska, Dawid Lisicki and Ewa Pankalla
Materials 2023, 16(17), 5778; https://doi.org/10.3390/ma16175778 - 23 Aug 2023
Cited by 3 | Viewed by 3158
Abstract
An efficient method for the synthesis of 2-ethylhexanoic acid has been reported. The method involves the 2-ethylhexanal oxidation using oxygen or air in the presence of N-hydroxyphthalimide in isobutanol as a solvent under mild conditions. A high selectivity of >99% for [...] Read more.
An efficient method for the synthesis of 2-ethylhexanoic acid has been reported. The method involves the 2-ethylhexanal oxidation using oxygen or air in the presence of N-hydroxyphthalimide in isobutanol as a solvent under mild conditions. A high selectivity of >99% for 2-ethylhexanoic acid was achieved. The influence of catalyst amount, solvent type and quantity, temperature, and reaction time on the product composition was studied. The developed method is in line with the global trends aimed at developing green oxidation processes as well as having potential for implementation in industry due to its high selectivity, cost-effective oxidizing agent, and mild reaction conditions. The use of isobutanol as a solvent is of crucial importance providing an opportunity for potential producers of 2-EHAL from butanal to employ the less valuable alcohol. Full article
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36 pages, 13691 KiB  
Review
Radical Decarboxylative Carbon–Nitrogen Bond Formation
by Xiangting Li, Xiaobin Yuan, Jiahao Hu, Yajun Li and Hongli Bao
Molecules 2023, 28(10), 4249; https://doi.org/10.3390/molecules28104249 - 22 May 2023
Cited by 17 | Viewed by 5149
Abstract
The carbon–nitrogen bond is one of the most prevalent chemical bonds in natural and artificial molecules, as many naturally existing organic molecules, pharmaceuticals, agrochemicals, and functional materials contain at least one nitrogen atom. Radical decarboxylative carbon–nitrogen bond formation from readily available carboxylic acids [...] Read more.
The carbon–nitrogen bond is one of the most prevalent chemical bonds in natural and artificial molecules, as many naturally existing organic molecules, pharmaceuticals, agrochemicals, and functional materials contain at least one nitrogen atom. Radical decarboxylative carbon–nitrogen bond formation from readily available carboxylic acids and their derivatives has emerged as an attractive and valuable tool in modern synthetic chemistry. The promising achievements in this research topic have been demonstrated via utilizing this strategy in the synthesis of complex natural products. In this review, we will cover carbon–nitrogen bond formation via radical decarboxylation of carboxylic acids, Barton esters, MPDOC esters, N–hydroxyphthalimide esters (NHP esters), oxime esters, aryliodine(III) dicarboxylates, and others, respectively. This review aims to bring readers a comprehensive survey of the development in this rapidly expanding field. We hope that this review will emphasize the knowledge, highlight the proposed mechanisms, and further disclose the fascinating features in modern synthetic applications. Full article
(This article belongs to the Section Organic Chemistry)
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17 pages, 4717 KiB  
Review
Ugi Four-Component Reactions Using Alternative Reactants
by Seyyed Emad Hooshmand and Wei Zhang
Molecules 2023, 28(4), 1642; https://doi.org/10.3390/molecules28041642 - 8 Feb 2023
Cited by 24 | Viewed by 9298
Abstract
The Ugi four-component reaction (Ugi-4CR) undoubtedly is the most prominent multicomponent reaction (MCRs) that has sparked organic chemists’ interest in the field. It has been widely used in the synthesis of diverse heterocycle molecules such as potential drugs, natural product analogs, pseudo peptides, [...] Read more.
The Ugi four-component reaction (Ugi-4CR) undoubtedly is the most prominent multicomponent reaction (MCRs) that has sparked organic chemists’ interest in the field. It has been widely used in the synthesis of diverse heterocycle molecules such as potential drugs, natural product analogs, pseudo peptides, macrocycles, and functional materials. The Ugi-4CRs involve the use of an amine, an aldehyde or ketone, an isocyanide, and a carboxylic acid to produce an α-acetamido carboxamide derivative, which has significantly advanced the field of isocyanide-based MCRs. The so-called intermediate nitrilium ion could be trapped by a nucleophile such as azide, N-hydroxyphthalimide, thiol, saccharin, phenol, water, and hydrogen sulfide instead of the original carboxylic acid to allow for a wide variety of Ugi-type reactions to occur.β In addition to isocyanide, there are alternative reagents for the other three components: amine, isocyanide, and aldehyde or ketone. All these alternative components render the Ugi reaction an aptly diversity-oriented synthesis of a myriad of biologically active molecules and complex scaffolds. Consequently, this review will delve deeper into alternative components used in the Ugi MCRs, particularly over the past ten years. Full article
(This article belongs to the Special Issue Green and Highly Efficient One-Pot Synthesis and Catalysis)
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17 pages, 1630 KiB  
Article
Heterogeneous Photocatalysis as a Potent Tool for Organic Synthesis: Cross-Dehydrogenative C–C Coupling of N-Heterocycles with Ethers Employing TiO2/N-Hydroxyphthalimide System under Visible Light
by Elena R. Lopat’eva, Igor B. Krylov, Oleg O. Segida, Valentina M. Merkulova, Alexey I. Ilovaisky and Alexander O. Terent’ev
Molecules 2023, 28(3), 934; https://doi.org/10.3390/molecules28030934 - 17 Jan 2023
Cited by 13 | Viewed by 3419
Abstract
Despite the obvious advantages of heterogeneous photocatalysts (availability, stability, recyclability, the ease of separation from products and safety) their application in organic synthesis faces serious challenges: generally low efficiency and selectivity compared to homogeneous photocatalytic systems. The development of strategies for improving the [...] Read more.
Despite the obvious advantages of heterogeneous photocatalysts (availability, stability, recyclability, the ease of separation from products and safety) their application in organic synthesis faces serious challenges: generally low efficiency and selectivity compared to homogeneous photocatalytic systems. The development of strategies for improving the catalytic properties of semiconductor materials is the key to their introduction into organic synthesis. In the present work, a hybrid photocatalytic system involving both heterogeneous catalyst (TiO2) and homogeneous organocatalyst (N-hydroxyphthalimide, NHPI) was proposed for the cross-dehydrogenative C–C coupling of electron-deficient N-heterocycles with ethers employing t-BuOOH as the terminal oxidant. It should be noted that each of the catalysts is completely ineffective when used separately under visible light in this transformation. The occurrence of visible light absorption upon the interaction of NHPI with the TiO2 surface and the generation of reactive phthalimide-N-oxyl (PINO) radicals upon irradiation with visible light are considered to be the main factors determining the high catalytic efficiency. The proposed method is suitable for the coupling of π-deficient pyridine, quinoline, pyrazine, and quinoxaline heteroarenes with various non-activated ethers. Full article
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19 pages, 1694 KiB  
Article
Photocatalyzed Oxidative Decarboxylation Forming Aminovinylcysteine Containing Peptides
by Masaya Kumashiro, Kosuke Ohsawa and Takayuki Doi
Catalysts 2022, 12(12), 1615; https://doi.org/10.3390/catal12121615 - 9 Dec 2022
Cited by 3 | Viewed by 3080
Abstract
The formation of (2S,3S)-S-[(Z)-aminovinyl]-3-methyl-D-cysteine (AviMeCys) substructures was developed based on the photocatalyzed-oxidative decarboxylation of lanthionine-bearing peptides. The decarboxylative selenoetherification of the N-hydroxyphthalimide ester, generated in situ, proceeded under mild conditions at −40 °C in [...] Read more.
The formation of (2S,3S)-S-[(Z)-aminovinyl]-3-methyl-D-cysteine (AviMeCys) substructures was developed based on the photocatalyzed-oxidative decarboxylation of lanthionine-bearing peptides. The decarboxylative selenoetherification of the N-hydroxyphthalimide ester, generated in situ, proceeded under mild conditions at −40 °C in the presence of 1 mol% of eosin Y-Na2 as a photocatalyst and the Hantzsch ester. The following β-elimination of the corresponding N,Se-acetal was operated in a one-pot operation, led to AviMeCys substructures found in natural products in moderate to good yields. The sulfide-bridged motif, and also the carbamate-type protecting groups, such as Cbz, Teoc, Boc and Fmoc groups, were tolerant under the reaction conditions. Full article
(This article belongs to the Special Issue Theme Issue in Memory to Prof. Jiro Tsuji (1927–2022))
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4 pages, 244 KiB  
Short Note
2-(2,5-Dimethoxyphenoxy)isoindoline-1,3-dione
by Stanislav A. Paveliev, Oleg O. Segida and Alexander O. Terent’ev
Molbank 2022, 2022(4), M1514; https://doi.org/10.3390/M1514 - 2 Dec 2022
Cited by 2 | Viewed by 1980
Abstract
In this work, the direct C-H functionalization reaction of 1,4-dimethoxybenzene with N-hydroxyphthalimide has been disclosed. A previously unknown product of the C-O coupling of 1,4-dimethoxybenzene and N-hydroxyphthalimide was obtained. The reaction proceeded under mild conditions, in which a commercially available manganese-based [...] Read more.
In this work, the direct C-H functionalization reaction of 1,4-dimethoxybenzene with N-hydroxyphthalimide has been disclosed. A previously unknown product of the C-O coupling of 1,4-dimethoxybenzene and N-hydroxyphthalimide was obtained. The reaction proceeded under mild conditions, in which a commercially available manganese-based oxidizing agent was used for generation of a phthalimide-N-oxyl radical. The obtained compound is a promising valuable precursor of O-aryl hydroxylamine. Full article
(This article belongs to the Section Organic Synthesis and Biosynthesis)
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16 pages, 5118 KiB  
Article
Selective Oxidation of Toluene to Benzaldehyde Using Co-ZIF Nano-Catalyst
by Wei Long, Zhilong Chen, Yinfei Huang and Xinping Kang
Int. J. Mol. Sci. 2022, 23(21), 12881; https://doi.org/10.3390/ijms232112881 - 25 Oct 2022
Cited by 6 | Viewed by 3778
Abstract
Nanometer-size Co-ZIF (zeolitic imidazolate frameworks) catalyst was prepared for selective oxidation of toluene to benzaldehyde under mild conditions. The typical characteristics of the metal-organic frameworks (MOFs) material were affirmed by the XRD, SEM, and TEM, the BET surface area of this catalyst was [...] Read more.
Nanometer-size Co-ZIF (zeolitic imidazolate frameworks) catalyst was prepared for selective oxidation of toluene to benzaldehyde under mild conditions. The typical characteristics of the metal-organic frameworks (MOFs) material were affirmed by the XRD, SEM, and TEM, the BET surface area of this catalyst was as high as 924.25 m2/g, and the diameter of particles was near 200 nm from TEM results. The Co metal was coated with 2-methyl glyoxaline, and the crystalline planes were relatively stable. The reaction temperatures, oxygen pressure, mass amount of N-hydroxyphthalimide (NHPI), and reaction time were discussed. The Co-ZIF catalyst gave the best result of 92.30% toluene conversion and 91.31% selectivity to benzaldehyde under 0.12 MPa and 313 K. The addition of a certain amount of NHPI and the smooth oxidate capacity of the catalyst were important factors in the high yield of benzaldehyde. This nanometer-size catalyst showed superior performance for recycling use in the oxidation of toluene. Finally, a possible reaction mechanism was proposed. This new nanometer-size Co-ZIF catalyst will be applied well in the selective oxidation of toluene to benzaldehyde. Full article
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13 pages, 3434 KiB  
Article
Pullulan Oxidation in the Presence of Hydrogen Peroxide and N-Hydroxyphthalimide
by Gabriela Biliuta, Raluca Ioana Baron and Sergiu Coseri
Materials 2022, 15(17), 6086; https://doi.org/10.3390/ma15176086 - 2 Sep 2022
Cited by 5 | Viewed by 2456
Abstract
The C-6 in the maltotriose unit of pullulan was oxidized in an alkaline medium (pH = 10), utilizing a green method that included hydrogen peroxide (H2O2) as an oxidant and N-hydroxyphthalimide (NHPI) as a catalyst for various reaction [...] Read more.
The C-6 in the maltotriose unit of pullulan was oxidized in an alkaline medium (pH = 10), utilizing a green method that included hydrogen peroxide (H2O2) as an oxidant and N-hydroxyphthalimide (NHPI) as a catalyst for various reaction times. The structure of the resulting oxidized pullulans (PO) was carefully characterized by titration, intrinsic viscosity, FTIR, 13C-NMR, and zeta potential. The content of carboxyl groups in PO was dependent on reaction time and varied accordingly. Furthermore, a fast reaction rate was found in the first 2–3 h of the reaction, followed by a decreased rate in the subsequent hours. FTIR and 13C-NMR proved that the selective oxidation of the primary alcohol groups of pullulan was achieved. The oxidation also caused the glycoside linkages in the pullulan chain to break, and the viscosity of the pullulan itself went down. Full article
(This article belongs to the Special Issue Advances in Nanostructured Catalysts)
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15 pages, 2453 KiB  
Article
Oxyfunctionalization of Benzylic C-H Bonds of Toluene Mediated by Covalently Anchored Co-Schiff Bases
by Guojun Shi, Yuxin Liang, Hongyu Zhou, Zhengliang Zhao and Wenjie Yang
Molecules 2022, 27(16), 5302; https://doi.org/10.3390/molecules27165302 - 19 Aug 2022
Cited by 3 | Viewed by 1801
Abstract
Oxyfunctionalization of toluene to value-added benzaldehyde, benzyl alcohol and benzoic acid is of great significance. In this work, Co-Schiff bases were immobilized on commercial silica gel by covalent anchoring, and resulting catalysts were used to catalyze the oxidation of toluene in the presence [...] Read more.
Oxyfunctionalization of toluene to value-added benzaldehyde, benzyl alcohol and benzoic acid is of great significance. In this work, Co-Schiff bases were immobilized on commercial silica gel by covalent anchoring, and resulting catalysts were used to catalyze the oxidation of toluene in the presence of the cocatalyst N-hydroxyphthalimide (NHPI). The catalysts exhibited excellent textural and structural properties, reliable bonding and a predomination of the cobaltous ions. The catalyst synthesized by diethylamino salicylaldehyde (EASA) possessed a grafting density of 0.14 mmol/g and exhibited a toluene conversion of 37.5%, with predominant selectivities to benzaldehyde, benzyl alcohol and benzoic acid under solvent-free conditions. It is concluded that the effect of ligands on their catalytic performance might be related to their electron-donating or -withdrawing properties. Full article
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19 pages, 4540 KiB  
Article
Selective Aerobic Oxidation of P-Methoxytoluene by Co(II)-Promoted NHPI Incorporated into Cross-Linked Copolymer Structure
by Tomasz Berniak, Piotr Łątka, Anna Rokicińska, Karol Sidor and Piotr Kuśtrowski
Catalysts 2021, 11(12), 1474; https://doi.org/10.3390/catal11121474 - 1 Dec 2021
Cited by 5 | Viewed by 3414
Abstract
A wide series of copolymer materials with various contents of 4-vinyl-diisopropyl-phtalate ester (10–90 mol%), divinylbenzene (1–11 mol%) and styrene, as monomers, were obtained by radical copolymerization. In the last steps of the synthesis, diisopropyl ester functionalities were converted into the form of N-hydroxyphthalimide [...] Read more.
A wide series of copolymer materials with various contents of 4-vinyl-diisopropyl-phtalate ester (10–90 mol%), divinylbenzene (1–11 mol%) and styrene, as monomers, were obtained by radical copolymerization. In the last steps of the synthesis, diisopropyl ester functionalities were converted into the form of N-hydroxyphthalimide (NHPI) rings. The obtained materials with the NHPI groups immobilized in the copolymer structure were studied by various physicochemical techniques, including FT-IR, UV-Vis-DR, XPS, elemental analysis, and tested as catalysts in aerobic oxidation of p-methoxytoluene in the presence of Co(II) acetate co-catalyst. Conversion of the aromatic substrate was correlated with the NHPI content and cross-linking degree. The best catalytic performance (conversions higher than 23%) was achieved for the copolymer catalysts containing 60% and 30% of 4-vinyl-diisopropyl-phtalate ester. At too high concentrations of NHPI and DVB, some of the NHPI groups were transformed into inactive (C=O)-N=O species or not available due to embedding inside the copolymer structure. The mechanism of the process involving both NHPI centers, forming phthalimide N-oxyl (PINO) radicals, and Co(II) cations was discussed. Stability of the developed catalysts was also tested. The opening of imide rings took place during the catalytic process, resulting in the formation of carboxyl groups and the release of hydroxylamine molecules. The deactivated catalyst could be easily regenerated by repeating two last steps of closing imide ring. Full article
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17 pages, 72752 KiB  
Article
Manganese-Doped N-Hydroxyphthalimide-Derived Carbon Dots—Theranostics Applications in Experimental Breast Cancer Models
by Adrian Tiron, Corneliu S. Stan, Gabriel Luta, Cristina M. Uritu, Irina-Cezara Vacarean-Trandafir, Gabriela D. Stanciu, Adina Coroaba and Crina E. Tiron
Pharmaceutics 2021, 13(11), 1982; https://doi.org/10.3390/pharmaceutics13111982 - 22 Nov 2021
Cited by 20 | Viewed by 3118
Abstract
Background: Theranostics, a novel concept in medicine, is based on the use of an agent for simultaneous diagnosis and treatment. Nanomaterials provide promising novel approaches to theranostics. Carbon Dots have been shown to exhibit anti-tumoral properties in various cancer models. The aim of [...] Read more.
Background: Theranostics, a novel concept in medicine, is based on the use of an agent for simultaneous diagnosis and treatment. Nanomaterials provide promising novel approaches to theranostics. Carbon Dots have been shown to exhibit anti-tumoral properties in various cancer models. The aim of the present study is to develop gadolinium, Fe3+, and Mn2+-doped N-hydroxyphthalimide-derived Carbon Dots. The resulted doped Carbon Dots should preserve the anti-tumoral properties while gaining magnetic resonance imaging properties. Methods: Normal and cancer cell lines have been treated with doped Carbon Dots, and the cell viability has been measured. The doped Carbon Dots that exhibited the most prominent anti-tumoral effect accompanied by the lowest toxicity have been further in vivo tested. Magnetic resonance imaging evaluates both in vitro and in vivo the possibility of using doped Carbon Dots as a contrast agent. Results: According to the results obtained from both the in vitro and in vivo experimental models used in our study, Mn2+-doped Carbon Dots (Mn-CDs-NHF) exhibit anti-tumoral properties, do not significantly impair the cell viability of normal cells, and reduce lung metastasis and the volume of mammary primary tumors while allowing magnetic resonance imaging. Conclusions: Our findings prove that Mn-CDs-NHF can be used as theranostics agents in pre-clinical models. Full article
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11 pages, 2080 KiB  
Article
Transition Metal Salts of Carboxylated Multiwalled Carbon Nanotubes in Combination with N-hydroxyphthalimide as Catalytic Systems for Hydrocarbon Oxidation
by Kamil Peckh and Beata Orlińska
Materials 2021, 14(9), 2314; https://doi.org/10.3390/ma14092314 - 29 Apr 2021
Cited by 5 | Viewed by 2172
Abstract
In this study, the transition metal (Co (II), Cu (II), and Mn (II)) salts of carboxylated carbon nanotubes were synthesized and characterized (the determined metal contents were in the range of 0.89–1.16%). The catalytic activity and the possibility for recovery and reuse of [...] Read more.
In this study, the transition metal (Co (II), Cu (II), and Mn (II)) salts of carboxylated carbon nanotubes were synthesized and characterized (the determined metal contents were in the range of 0.89–1.16%). The catalytic activity and the possibility for recovery and reuse of the obtained heterogeneous salts were then studied in the solvent-free oxidation of ethylbenzene with oxygen. The oxidation processes were carried out at 80 °C under atmospheric pressure in the presence of N-hydroxyphthalimide. The highest conversion of ethylbenzene, 27%, was obtained with a system consisting of the Cu (II) salt of the carboxylated carbon nanotubes, N-hydroxyphthalimide, and the azo initiator AIBN. Full article
(This article belongs to the Section Catalytic Materials)
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14 pages, 3816 KiB  
Article
Enhancing Anti-Tumoral Potential of CD-NHF by Modulating PI3K/Akt Axis in U87 Ex Vivo Glioma Model
by Gabriel Luta, Mihail Butura, Adrian Tiron and Crina E. Tiron
Int. J. Mol. Sci. 2021, 22(8), 3873; https://doi.org/10.3390/ijms22083873 - 8 Apr 2021
Cited by 3 | Viewed by 2889
Abstract
Background: In the latest years, there has been an increased interest in nanomaterials that may provide promising novel approaches to disease diagnostics and therapeutics. Our previous results demonstrated that Carbon-dots prepared from N-hydroxyphthalimide (CD-NHF) exhibited anti-tumoral activity on several cancer cell lines [...] Read more.
Background: In the latest years, there has been an increased interest in nanomaterials that may provide promising novel approaches to disease diagnostics and therapeutics. Our previous results demonstrated that Carbon-dots prepared from N-hydroxyphthalimide (CD-NHF) exhibited anti-tumoral activity on several cancer cell lines such as MDA-MB-231, A375, A549, and RPMI8226, while U87 glioma tumor cells were unaffected. Gliomas represent one of the most common types of human primary brain tumors and are responsible for the majority of deaths. In the present in vitro study, we expand our previous investigation on CD-NHF in the U87 cell line by adding different drug combinations. Methods: Cell viability, migration, invasion, and immunofluorescent staining of key molecular pathways have been assessed after various treatments with CD-NHF and/or K252A and AKTVIII inhibitors in the U87 cell line. Results: Association of an inhibitor strongly potentiates the anti-tumoral properties of CD-NHF identified by significant impairment of migration, invasion, and expression levels of phosphorylated Akt, p70S6Kinase, or by decreasing expression levels of Bcl-2, IL-6, STAT3, and Slug. Conclusions: Using simultaneously reduced doses of both CD-NHF and an inhibitor in order to reduce side effects, the viability and invasiveness of U87 glioma cells were significantly impaired. Full article
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