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1.
Chem Commun (Camb) ; 58(81): 11430-11433, 2022 Oct 11.
Artículo en Inglés | MEDLINE | ID: mdl-36134562

RESUMEN

A novel thio-Ritter-type reaction of alkyl bromides, nitriles, and hydrogen sulfide has been explored, providing a straightforward approach toward functionally important thioamides. This transformation features a broad substrate scope, operational simplicity, use of available feedstock chemicals, and late-stage functionalizations of bioactive molecules. The reaction mechanism is also proposed.


Asunto(s)
Sulfuro de Hidrógeno , Tioamidas , Bromuros , Estructura Molecular , Nitrilos/química , Tioamidas/química
2.
Chem Commun (Camb) ; 57(16): 2069-2072, 2021 Feb 25.
Artículo en Inglés | MEDLINE | ID: mdl-33507188

RESUMEN

Commercially available cinchona alkaloids that can catalyze the enantiodivergent fluorination of ß-ketodiarylphosphine oxides were developed to construct carbon-fluorine quaternary stereocenters. This protocol features a wide scope of substrates and excellent enantioselectivities, and it is scalable.

3.
Chin Med J (Engl) ; 121(16): 1563-8, 2008 Aug 20.
Artículo en Inglés | MEDLINE | ID: mdl-18982869

RESUMEN

BACKGROUND: Recent studies indicate that S100P expression may be a biomarker that can predict the success of cancer chemotherapy. Whether it is relevant to chemotherapeutics in ovarian cancer is unknown. In this study, we investigated the association of S100P expression with paclitaxel sensitivity in ovarian cancer cell lines. METHODS: We measured S100P expression and paclitaxel resistance profiles in parent SKOV3 and OVCAR3 cell lines. Then, the two cell lines were transiently transfected with S100P siRNA. We also constructed an OVCAR3 cell clone that stably overexpressed S100P. The effect of S100P expression level on the survival of cells exposed to paclitaxel was measured using the MTT assay. S100P expression was evaluated by semi-quantitative RT-PCR and Western blotting. Significance of differences was calculated using independent samples t-test and one way analysis of variance (ANOVA). RESULTS: Lower S100P expression was associated with a survival advantage in OVCAR3 cells exposed to paclitaxel; the survival advantage in SKOV3 cells was smaller (P < 0.05). The survival advantage associated with decreased S100P expression was even greater for SKOV3 and OVCAR3 cells that had been transfected with S100P siRNA before being exposed to paclitaxel (P < 0.05). Consistent with this, the OVCAR3 cell clone that was transfected to overexpress S100P was more sensitive to paclitaxel (P < 0.05). CONCLUSIONS: Low S100P expression contributes to drug resistance to paclitaxel in ovarian cancer cell lines. S100P expression thus might be a marker that can predict the effectiveness of paclitaxel based chemotherapy. Such a marker could be helpful in improving individual medication regimens for ovarian cancer patients.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Neoplasias Ováricas/tratamiento farmacológico , Paclitaxel/farmacología , Proteínas S100/fisiología , Línea Celular Tumoral , Supervivencia Celular , Resistencia a Antineoplásicos , Femenino , Humanos , Neoplasias Ováricas/patología , Proteínas S100/genética , Transfección
4.
Chin Med J (Engl) ; 121(15): 1398-406, 2008 Aug 05.
Artículo en Inglés | MEDLINE | ID: mdl-18959117

RESUMEN

BACKGROUND: For cardiovascular tissue engineering, acellularized biomaterials from pig have been widely investigated. Our purpose was to study mechanical properties and biocompatibility of decellularized aorta of fetal pigs (DAFP) to determine its potential as scaffold for small diameter tissue engineered vascular graft. METHODS: Descending aorta of fetal pigs was removed cells using trypsin, ribonuclease and desoxyribonuclease. Mechanical properties of DAFP were evaluated by tensile stress-strain and burst pressure analysis. Assessment of cell adhesion and compatibility was conducted by seeding porcine aortic endothelial cells. To evaluate biocompatibility in vivo, DAFP was implanted subcutaneously into adult male Sprague Dawley rats for 2, 4 and 8 weeks. RESULTS: Histochemistry and scanning electron microscopy examination of DAFP revealed well-preserved extracellular matrix proteins and porous three-dimensional structures. Compared with fresh aorta, DAFP had similar ultimate tensile strength, axial compliance and burst pressure. Cell culture studies in vitro showed that porcine aortic endothelial cells adhered and proliferated on the surfaces of DAFP with excellent cell viability. Subdermal implantation demonstrated that the DAFP did not show almost any immunological reaction and exhibited minimal calcification during the whole follow-up period. CONCLUSION: The DAFP has the potential to serve as scaffolds for small diameter tissue engineered vascular graft.


Asunto(s)
Aorta/citología , Prótesis Vascular , Ingeniería de Tejidos/métodos , Animales , Fenómenos Biomecánicos , Antígenos CD4/análisis , Calcio/metabolismo , Células Cultivadas , Matriz Extracelular/fisiología , Ensayo de Materiales , Porcinos
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