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Herein, we report a blue visible-light-promoted approach for preparing a variety of α-substituted γ-ketoester derivatives through carbene insertion and the decarbonylation of enaminones and diazoesters. These reactions use readily available starting materials and transition-metal-free, eco-friendly procedures that are amenable to gram-scale synthesis and wide functional group tolerance. This methodology may be useful for constructing polysubstituted heterocycles with potential biological activity.
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Luz , Metano , Metano/análogos & derivadosRESUMEN
A catalyst-free method for the highly regioselective hydrated ring-opening and formylation of quinazolinones was developed. This reaction realized the direct arylation of two nitrogen atoms on quinazolinones and realized the regioselective ring-opening of quinazolinone and subsequent acylation of methyleneamine through the nucleophilic addition of a water molecule to an imine carbon atom. It showed reasonable functional group compatibility and provided one-pot access to a variety of N-arylformyl derivatives in moderate to excellent yields.
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Carbono , Quinazolinonas , Catálisis , Nitrógeno , AguaRESUMEN
OBJECTIVE: Many acupuncture acupoints are located on the posterior midline of the neck region. The needling depth for acupuncture is important for practitioners, and an unsafe needling depth increases the possibility of damage to the spinal cord and brainstem. Can the safety of acupuncture be assessed by examining bone structures? We focused on this aim to carry out this study. METHODS: The shortest distance from the posterior border of the foramen magnum to the line joining both upper ends of the posterior border of the mastoid process was measured on 29 skulls. Distances from the posterior border of the vertebral foramen to the tip of the spinous process and posterior tubercle of the atlas were measured and evaluated from 197 dry cervical vertebrae and 31 lateral cervical radiographs of patient subjects. The anatomic relationships of the vertebral canal with the external occipital protuberance, tip of the spinous process of the axis, tip of the posterior tubercle of the atlas, and upper end of the posterior border of the mastoid process were observed and evaluated via lateral cervical radiography. RESULTS: The shortest distance from the foramen magnum to the line between the mastoid processes was 4.65±1.75 mm, and the distance from the superior border of the vertebral foramen of the atlas to the posterior tubercle was less than the distance from the inferior border. The distance from the superior border of the vertebral canal to the tip of the spinous process in C2-C7 was greater than the distance from the inferior border. The mean lengths of the superior border of the C2 spinous process and the inferior border of the C7 spinous process were greater than 21 mm and 31 mm, respectively. The line from the upper end of the posterior border of the mastoid process to the tip of the C2 spinous process or 10 mm deep to the tip of the C2 spinous process was posterior to the vertebral canal. CONCLUSIONS: On the posterior midline of the neck region between the tip of spinous process of axis and external occipital protuberance, if the needle reaches the depth of the line between the upper end of posterior border of mastoid process and the tip of the spinous process of the axis, approximately 10 mm along the spinous process of the axis, the needle is in the safe region. The mean length of the C2-C7 spinous process is suitable to accommodate the needling depth of the adjacent acupoint. Bone structures can be used to effectively assess the safety of acupuncture on the posterior midline of the neck region.
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Puntos de Acupuntura , Terapia por Acupuntura , Humanos , Masculino , Femenino , Terapia por Acupuntura/métodos , Adulto , Persona de Mediana Edad , Vértebras Cervicales , Puntos Anatómicos de Referencia , Cuello , Adulto Joven , AncianoRESUMEN
Following the publication of this paper, it was drawn to the Editors' attention by a concerned reader that various panels showing cell migration assay data in Figs. 3B and C and 5C and D were strikingly similar to data appearing in different form in other articles by different authors. Furthermore, overlapping data panels were identified within this paper comparing the cell migration assay images between Figs. 3B and 5C. Owing to the fact that the contentious data in the above article had already been published elsewhere, or were already under consideration for publication, prior to its submission to Molecular Medicine Reports, the Editor has decided that this paper should be retracted from the Journal. The authors were asked for an explanation to account for these concerns, but the Editorial Office did not receive a reply. The Editor apologizes to the readership for any inconvenience caused. [Molecular Medicine Reports 16: 36063612, 2017; DOI: 10.3892/mmr.2017.6968].
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Herein, we describe the dual C(sp3)-H bond functionalization of a tertiary amine through hydride-transfer-induced dehydrogenation, followed by cycloaddition, using an easily preparable diazoester as a new type hydride-acceptor precursor under mild, redox-neutral conditions. With carbene as a hydrogen acceptor, this method was demonstrated by the preparation of a broad range of functionalized isoxazoldines in moderate to good yields.
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Osteosarcoma (OS) is the most common malignant bone tumor in children and adolescents. microRNAs (miRNAs) have previously been reported to be involved in the carcinogenesis and progression of OS, and may be useful prognostic markers or therapeutic targets for patients with OS. miRNA130a has been previously studied in multiple types of human cancer. However, its expression and function in OS has not been well documented. The aim of the present study was to investigate the expression, biological functions and molecular mechanisms underlying the effect of miR130a in OS. miR130a was significantly downregulated in OS tissues and cell lines compared with normal bone tissue and a normal osteoblast cell line. miR130a expression levels was significantly negatively correlated with the clinical stage and metastasis of OS. Further studies indicated that overexpression of miR130a inhibited OS cell proliferation, migration and invasion in vivo. In terms of the mechanisms underlying this effect, zinc finger Ebox binding homeobox 1 (ZEB1) was demonstrated to act as a direct target of miR130a in OS. Furthermore, downregulation of ZEB1 by interference with small interfering RNA mimicked the effects of transfection with an miR130a mimic in OS. In conclusion, these results demonstrated that miR130a functioned as a tumor suppressor in OS, partially via targeting ZEB1, suggesting that miR130a may be considered as a target for the treatment of patients with OS.