- Synthesis and biological evaluation of new antioxidant and antiproliferative chalcogenobiotin derivatives for bladder carcinoma treatment
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Approximately 90% of bladder carcinomas are of the urothelial carcinoma type, which are characterized by high rates of recurrence and predisposition to progress to invasive tumors, representing one of the most costly neoplasms for health systems. Intraves
- Collares, Tiago,Dornelles, Luciano,Leitemberger, Andrielli,Nogara, Pablo A.,Piccoli, Bruna C.,Rodrigues, Oscar E. D.,Schachtschneider, Kyle M.,Seixas, Fabiana K.,Sonego, Mariana S.,da Silva, Fernanda D.,dos Santos, Alana C. F.,Garcia, Fábio D.,Oliveira, Cláudia S.,Rocha, Jo?o B. T.
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- Design, synthesis and biological evaluation of novel semicarbazone-selenochroman-4-ones hybrids as potent antifungal agents
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A series of novel 2,3-dihydro-4H-1-benzoselenin-4-one (thio)semicarbazone derivatives were designed and synthesized by using molecular hybridization approach. All the target compounds were characterized by HRMS and NMR and evaluated in vitro antifungal activity against five pathogenic strains. In comparison with precursor selenochroman-4-ones, the hybrid molecules in this study showed significant improvement in antifungal activities. Notably, compound B8 showed significant antifungal activity against other strains excluding Aspergillus fumigatus (0.25 μg/mL on Candida albicans, 2 μg/mL on Cryptococcus neoformans, 8 μg/mL on Candida zeylanoides and 2 μg/mL on fluconazole-sensitive strains of Candida albicans). Moreover, compounds B8, B9 and C2 also displayed most potent activities against four fluconazole-resistance strains. Especially the MIC values of the hybrid molecule B8 against fluconazole-resistant strains were in the range of 0.5–2 μg/mL. Therefore, the molecular hybridization approach in this study provided new ideas for the development of antifungal drug.
- Xu, Hang,Su, Xin,Liu, Xiao-qian,Zhang, Kai-peng,Hou, Zhuang,Guo, Chun
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supporting information
(2019/10/19)
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- Evidence for a common selenolate intermediate in the glutathione peroxidase-like catalysis of α-(phenylselenenyl) ketones and diphenyl diselenide
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The glutathione peroxidase-like catalysis of α-(phenylselenenyl) ketones was investigated. Degradation studies demonstrated the rapid cleavage of the aliphatic carbon-selenium bond of α-(phenylselenenyl) ketones by glutathione at pH 6.9 in a methanolic phosphate buffer under argon. On treatment with excess glutathione under aerobic conditions, α-(phenylselenenyl) ketones, S- (phenylselenenyl)glutathione and diphenyl diselenide were all shown to give benzeneselenolate. This material was found to be oxidized by hydrogen peroxide considerably faster than α-(phenylselenenyl) ketones, S- (phenylselenenyl)glutathione or diphenyl diselenide. A catalytic mechanism involving benzeneselenolate, benzeneselenenic acid and S- (phenylselenenyl)glutathione as crucial intermediates was proposed to account for the glutathione peroxidase-like catalysis of α-(phenylselenenyl) ketones and diphenyl diselenide.
- Engman, Lars,Andersson, Claes,Morgenstern, Ralf,Cotgreave, Ian A.,Andersson, Carl-Magnus,Hallberg, Anders
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p. 2929 - 2938
(2007/10/02)
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