| 1. |
- Chu, Dinh-Toi, et al.
(författare)
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An update on obesity : Mental consequences and psychological interventions
- 2019
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Ingår i: Diabetes & Metabolic syndrome. - : Elsevier. - 1871-4021 .- 1878-0334. ; 13:1, s. 155-160
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Forskningsöversikt (refereegranskat)abstract
- Besides physical consequences, obesity has negative psychological effects, thereby lowering human life quality. Major psychological consequences of this disorder includes depression, impaired body image, low self-esteem, eating disorders, stress and poor quality of life, which are correlated with age and gender. Physical interventions, mainly diet control and energy balance, have been widely applied to treat obesity; and some psychological interventions including behavioral therapy, cognitive behavioral therapy and hypnotherapy have showed some effects on obesity treatment. Other psychological therapies, such as relaxation and psychodynamic therapies, are paid less attention. This review aims to update scientific evidence regarding the mental consequences and psychological interventions for obesity. (c) 2018 Diabetes India. Published by Elsevier Ltd. All rights reserved.
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| 2. |
- Thanh Le, Thanh, et al.
(författare)
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Diarylether-Amino Acid Conjugates as New Class of Anticancer Agents
- 2023
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Ingår i: CHEMISTRYSELECT. - : Wiley. - 2365-6549. ; 8:28
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Tidskriftsartikel (refereegranskat)abstract
- Diarylether (DE) is a privileged structure found in both natural products and synthetic compounds including small molecule drugs. We present the synthesis of a series of 13 new DE-amino acid conjugates which were screened for cancer cells antiproliferation activity. Structure-activity relationship suggests ester and phenyl groups in DE-Phe-OEt 4 c are important for the activity. Compound 4 c inhibited strongly MCF-7 3D tumor sphere formation and have favourable calculated physical chemical properties according to Lipinski's rule of 5. Docking study suggests estrogen receptor and/ or 3a-HSD type 3 protein could be the target(s) for anticancer activity of this class of compounds.
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| 3. |
- Pham, Em Canh, et al.
(författare)
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N,2,6-Trisubstituted 1H-benzimidazole derivatives as a new scaffold of antimicrobial and anticancer agents : design, synthesis, in vitro evaluation, and in silico studies
- 2023
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Ingår i: RSC Advances. - : Royal Society of Chemistry. - 2046-2069. ; 13:1, s. 399-420
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Tidskriftsartikel (refereegranskat)abstract
- Compounds containing benzimidazole moiety occupy privileged chemical space for discovering new bioactive substances. In continuation of our recent work, 69 benzimidazole derivatives were designed and synthesized with good to excellent yields of 46-99% using efficient synthesis protocol i.e. sodium metabisulfite catalyzed condensation of aromatic aldehydes with o-phenylenediamines to form 2-arylbenzimidazole derivatives followed by N-alkylation by conventional heating or microwave irradiation for diversification. Potent antibacterial compounds against MSSA and MRSA were discovered such as benzimidazole compounds 3k (2-(4-nitrophenyl), N-benzyl), 3l (2-(4-chlorophenyl), N-(4-chlorobenzyl)), 4c (2-(4-chlorophenyl), 6-methyl, N-benzyl), 4g (2-(4-nitrophenyl), 6-methyl, N-benzyl), and 4j (2-(4-nitrophenyl), 6-methyl, N-(4-chlorobenzyl)) with MIC of 4-16 mu g mL(-1). In addition, compound 4c showed good antimicrobial activities (MIC = 16 mu g mL(-1)) against the bacteria strains Escherichia coli and Streptococcus faecalis. Moreover, compounds 3k, 3l, 4c, 4g, and 4j have been found to kill HepG2, MDA-MB-231, MCF7, RMS, and C26 cancer cells with low mu M IC50 (2.39-10.95). These compounds showed comparable drug-like properties as ciprofloxacin, fluconazole, and paclitaxel in computational ADMET profiling. Finally, docking studies were used to assess potential protein targets responsible for their biological activities. Especially, we found that DHFR is a promising target both in silico and in vitro with compound 4c having IC50 of 2.35 mu M.
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| 4. |
- Tai, Thai Duy Phuoc, et al.
(författare)
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Synthesis of new 1,2,3-triazole derivatives from vanillin and beta-naphthol
- 2019
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Ingår i: VIETNAM JOURNAL OF CHEMISTRY. - : WILEY. - 0866-7144 .- 2572-8288. ; 57:1, s. 116-120
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Tidskriftsartikel (refereegranskat)abstract
- We herein report the synthesis of two new 1,2,3-triazole derivatives from vanillin and beta-naphthol. These 1,2,3-triazoles contain the diaryl ether moiety which has been synthesized via SNAr reaction under mild conditions and in excellent yields. Chemical structures of these triazoles were elucidated by spectroscopic analyses (HR-MS, NMR, IR).
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| 5. |
- Ballante, Flavio, et al.
(författare)
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Docking Finds GPCR Ligands in Dark Chemical Matter
- 2020
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Ingår i: Journal of Medicinal Chemistry. - : American Chemical Society (ACS). - 0022-2623 .- 1520-4804. ; 63:2, s. 613-620
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Tidskriftsartikel (refereegranskat)abstract
- High-throughput screening has revealed dark chemical matter, a set of drug-like compounds that has never shown bioactivity despite being extensively assayed. If dark molecules are found active at a therapeutic target, their extraordinary selectivity profiles make excellent starting points for drug development. We explored if ligands of therapeutically relevant G-protein-coupled receptors could be discovered by structure-based virtual screening of the dark chemical matter. Molecular docking screens against crystal structures of the A(2A) adenosine and the D-4 dopamine receptors were carried out, and 53 top-ranked molecules were evaluated experimentally. Two ligands of each receptor were discovered, and the most potent had sub-micromolar affinities. Analysis of bioactivity data showed that the ligands lacked activity at hundreds of off-targets, including several that are associated with adverse effects. Our results demonstrate that virtual screening provides an efficient means to mine the dark chemical space, which could contribute to development of drugs with improved safety profiles.
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| 6. |
- Bonagas, Nadilly, et al.
(författare)
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Pharmacological targeting of MTHFD2 suppresses acute myeloid leukemia by inducing thymidine depletion and replication stress
- 2022
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Ingår i: NATURE CANCER. - : Springer Science and Business Media LLC. - 2662-1347. ; 3:2, s. 156-
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Tidskriftsartikel (refereegranskat)abstract
- The folate metabolism enzyme MTHFD2 (methylenetetrahydrofolate dehydrogenase/cyclohydrolase) is consistently overexpressed in cancer but its roles are not fully characterized, and current candidate inhibitors have limited potency for clinical development. In the present study, we demonstrate a role for MTHFD2 in DNA replication and genomic stability in cancer cells, and perform a drug screen to identify potent and selective nanomolar MTHFD2 inhibitors; protein cocrystal structures demonstrated binding to the active site of MTHFD2 and target engagement. MTHFD2 inhibitors reduced replication fork speed and induced replication stress followed by S-phase arrest and apoptosis of acute myeloid leukemia cells in vitro and in vivo, with a therapeutic window spanning four orders of magnitude compared with nontumorigenic cells. Mechanistically, MTHFD2 inhibitors prevented thymidine production leading to misincorporation of uracil into DNA and replication stress. Overall, these results demonstrate a functional link between MTHFD2-dependent cancer metabolism and replication stress that can be exploited therapeutically with this new class of inhibitors. Helleday and colleagues describe a nanomolar MTHFD2 inhibitor that causes replication stress and DNA damage accumulation in cancer cells via thymidine depletion, demonstrating a potential therapeutic strategy in AML tumors in vivo.
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| 7. |
- Bui, Hue Thi Buu, et al.
(författare)
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Microwave assisted synthesis and cytotoxic activity evaluations of new benzimidazole derivatives
- 2016
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Ingår i: Tetrahedron Letters. - : Elsevier. - 0040-4039 .- 1359-8562. ; 57:8, s. 887-891
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Tidskriftsartikel (refereegranskat)abstract
- Twelve new 2-quinolizinylbenzimidazole and 2-naphthalylbenzimidazole derivatives with various 5- and 6-positioned substituents (aza, H, CH3, Cl, NO2, NH2, OCH3), have been synthesized in moderate to excellent yields via the condensation of 4-oxo-4H-quinolizinecarbaldehyde or naphthalenecarbaldehyde with substituted o-phenylenediamines, o-nitroaniline, and 2,3-pyridinediamine using sodium metabisulfite or sodium hydrosulfite under microwave irradiation. The new benzimidazole derivatives were screened for their cytotoxic activity against the human breast cancer cell line (MCF-7). The results showed on one hand that 2-(substituted quinolizinyl)-1H-benzimidazoles (12b–f) were less active (3–6 fold) than the positive control Tamoxifen (CC50 = 6.52 μM), and on the other hand, among the 2-(substituted naphthalyl)-1H-benzimidazoles series (13a–f), compounds 6,7,8-trimethoxy-3-(5-chloro-1H-benzo[d]imidazol-2-yl)naphthalen-1-ol (13c) (CC50 = 7.48 μM) and 6,7,8-trimethoxy-3-(5-methoxy-1H-benzo[d]imidazol-2-yl)naphthalen-1-ol (13f) (CC50 = 6.43 μM) were found to be as active as Tamoxifen.
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| 8. |
- Duoc, Vo Thanh, et al.
(författare)
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Hydrogen gas sensor based on self-heating effect of SnO2/Pt thin film with ultralow power consumption
- 2024
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Ingår i: International journal of hydrogen energy. - : Elsevier. - 0360-3199 .- 1879-3487. ; 61, s. 774-782
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Tidskriftsartikel (refereegranskat)abstract
- Self-heating of sensing elements on gas sensors is an effective solution to avoid using external heaters. In this paper, a self-heated hydrogen gas sensor is presented. The sensor was created using the DC sputtering method, which involved fabricating it on a thermal-insulating Kapton flexible substrate. This process utilized a thin film of SnO2 with thick 50 nm that was modified with nanoclusters of Pt, serving as the sensing material. The SnO2/Pt material film was analyzed for microstructure and composition by SEM, XRD, and XPS analysis. Infrared images show that the self-heating effect is mainly concentrated in the strip of gas-sensitive material. It showed many good performances, such as high sensitivity (able to detect down to 50 ppm of H2), good selectivity (poor response to CO, NH3, H2S, and NO2), the sensor's performance is little changed by environmental humidity, and low power consumption (89 μW at 5V). The sensor is also stable and low-cost, suitable for portable H2 detection devices due to its low generated heat and small size.
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| 9. |
- Duoc, Vo Thanh, et al.
(författare)
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New Design of ZnO Nanorod- and Nanowire-Based NO2 Room-Temperature Sensors Prepared by Hydrothermal Method
- 2019
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Ingår i: Journal of Nanomaterials. - : HINDAWI LTD. - 1687-4110 .- 1687-4129.
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Tidskriftsartikel (refereegranskat)abstract
- Room-temperature gas sensors are attracting attention because of their low power consumption, safe operation, and long-term stability. Herein, ZnO nanorods (NRs) and nanowires (NWs) were on-chip grown via a facile hydrothermal method and used for room-temperature NO2 gas sensor applications. The ZnO NRs were obtained by a one-step hydrothermal process, whereas the NWs were obtained by a two-step hydrothermal process. To obtain ZnO NW sensor, the length of NRs was controlled short enough so that none of the nanorod-nanorod junction was made. Thereafter, the NWs were grown from the tips of no-contact NRs to form nanowire-nanowire junctions. The gas-sensing characteristics of ZnO NRs and NWs were tested against NO2 gas at room temperature for comparison. The gas-sensing characteristics of the sensors were also tested at different applied voltages to evaluate the effect of the self-activated gas-sensing performance. Results show that the diameter of ZnO NRs and NWs is the dominant parameter of their NO2 gas-sensing performance at room temperature. In addition, self-activation by local heating occurred for both sensors, but because the NWs were smaller and sparser than the NRs, local heating thus required a lower applied voltage with maximal response compared with the NRs.
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| 10. |
- Duoc, Vo Thanh, et al.
(författare)
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Room temperature highly toxic NO2 gas sensors based on rootstock/scion nanowires of SnO2/ZnO, ZnO/SnO2, SnO2/SnO2 and, ZnO/ZnO
- 2021
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Ingår i: Sensors and actuators. B, Chemical. - : Elsevier. - 0925-4005 .- 1873-3077. ; 348
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Tidskriftsartikel (refereegranskat)abstract
- Grafted structures between SnO2 and ZnO nanowires were realized in a two-step process of growth. First, the rootstocks of SnO2 or ZnO nanowires were synthesized by thermal evaporation technique. Second, a thin Au layer was sputter deposited on the sample and synthesis of nanowire scions of ZnO or SnO2, respectively, on the rootstocks was realized by thermal evaporation technique again. In both growth steps, SnO2 powder or a mixture of ZnO and carbon powders was use as source materials for the synthesis. Different rootstock/scion combinations of SnO2/ZnO, ZnO/SnO2 nanowires (called heterostructures) and ZnO/ZnO, SnO2/SnO2 nanowires (called homostructures) were synthesised. The fabricated grafted nanowires were examined by field-emission scanning electron microscope and their compositions were analyzed by energy dispersive spectroscopy and X-ray diffraction analysis. The test results indicate that this type of nanostructure material is very promising for NO2 gas sensing at ppt level at room temperature. Among the fabricated structures the SnO2/ZnO nanowires showed the best sensing performance with the high sensitivity and fast response and recovery time. We also discussed the gas sensing mechanism of the fabricated sensors based on the band diagram.
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