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#1Nelly Durand (CNRS: Centre national de la recherche scientifique)H-Index: 8
Last. Isabelle Mus-VeteauH-Index: 15
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We previously reported that methiothepin, a small molecule known as a nonselective serotonin 5-HT receptor antagonist, inhibited the doxorubicin efflux activity of the Hedgehog receptor Ptch1 and enhanced the cytotoxic, pro-apoptotic, anti-proliferative, and anti-clonogenic effects of doxorubicin on adrenocortical carcinoma cells. Here, we show that methiothepin also inhibits doxorubicin efflux and increases doxorubicin cytotoxicity in melanoma cells which endogenously overexpress Ptch1. Melanom...
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#2Jong-Hoon KimH-Index: 16
Last. Eunha Kim
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Various bioorthogonal chemistries have been used for fluorescent imaging owing to the advantageous reactions they employ. Recent advances in bioorthogonal chemistry have revolutionized labeling strategies for fluorescence imaging, with inverse electron demand Diels–Alder (iEDDA) reactions in particular attracting recent attention owing to their fast kinetics and excellent specificity. One of the most interesting features of the iEDDA labeling strategy is that tetrazine-functionalized dyes are kn...
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#1Jakub WantulokH-Index: 2
#2Daniel SwobodaH-Index: 1
Last. Vladimír KubíčekH-Index: 11
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The vicarious nucleophilic substitution of hydrogen (VNS) reaction in electron-deficient nitroquinolines was studied. Properties of all new products have been characterized by several techniques: MS, HRMS, FTIR, GC-MS, electronic absorption spectroscopy, and multinuclear NMR. The structures of 4-chloro-8-nitroquinoline, 8-(tert-butyl)-2-methyl-5-nitroquinoline, 9-(8-nitroquinolin-7-yl)-9H-carbazole and (Z)-7-(9H-carbazol-9-yl)-8-(hydroxyimino)quinolin-5(8H)-one were determined by single-crystal ...
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#2Mahmoud YounsH-Index: 18
Last. Ahmed M. SaidH-Index: 4
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Scaffolds hybridization is a well-known drug design strategy for antitumor agents. Herein, series of novel indolyl-pyrimidine hybrids were synthesized and evaluated in vitro and in vivo for their antitumor activity. The in vitro antiproliferative activity of all compounds was obtained against MCF-7, HepG2, and HCT-116 cancer cell lines, as well as against WI38 normal cells using the resazurin assay. Compounds 1–4 showed broad spectrum cytotoxic activity against all these cancer cell lines compar...
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Undirected modifications between food proteins and secondary plant metabolites can occur during food processing. The results of covalent interactions can alter the functional and biological properties of the proteins. The present work studied the extent of which covalent conjugation of the bioactive metabolite benzyl isothiocyanate (BITC; a glucosinolate breakdown product) to the whey protein α-lactalbumin affects the protein’s allergenicity. Additional to the immunological analysis of native un...
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#1Nieves BaenasH-Index: 17
Last. F. J. García-AlonsoH-Index: 7
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Different strategies have been developed to increase the concentration of bioactive compounds in tomatoes during post-harvest, with ultraviolet light (UV) and light emitting diodes (LEDs) being interesting tools. The aim of this study was to evaluate the effect of ultraviolet (UVA at 366 nm and UVC at 254 nm) pre-treatment (1 kJ/m2) and red–blue LED light (25.4 µmol/m2/s) on the concentration of carotenoids, (poly)phenols and hydrophilic/lipophilic antioxidant capacity during 7 days of refrigera...
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#1Marek KieliszekH-Index: 19
#2Katarzyna PobiegaH-Index: 8
Last. Anna M. KotH-Index: 11
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Over the past several decades, we have observed a very rapid development in the biotechnological use of lactic acid bacteria (LAB) in various branches of the food industry. All such areas of activity of these bacteria are very important and promise enormous economic and industrial successes. LAB are a numerous group of microorganisms that have the ability to ferment sugars into lactic acid and to produce proteolytic enzymes. LAB proteolytic enzymes play an important role in supplying cells with ...
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The photochemical behavior of the photosensitive first-line anticancer drug vemurafenib (VFB) is of great interest due to the impact of such behavior on its pharmacological activity. In this work, we computationally elucidated the mechanism of the photoinduced release of VFB from the 4,5-dimethoxy-2-nitrobenzene (DMNB) photoprotecting group by employing various density functional theory (DFT)/time-dependent DFT (TD-DFT) approaches. The computational investigations included a comparative assessme...
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High-pressure synthesis and crystal structures of the homologous series AuBa2(Ca,Ln)n−1CunO2n+3 (n = 1–4; Ln = rare-earth cations) are described. Their crystal structures and superconducting properties are compared with the corresponding members of the Hg-homologous series. Numerous cuprates containing flat structural fragments (CuO4, CO3 and BO3) synthesized mainly at high pressure are compared in terms of structural peculiarities and superconducting properties. Importance and future prospects ...
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#1Sören ArltH-Index: 1
#2Vladana PetkovicH-Index: 3
Last. Goran N. KaluđerovićH-Index: 27
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Neutral [Ru(η6-arene)Cl2{Ph2P(CH2)3SPh-κP}] (arene = benzene, indane, 1,2,3,4-tetrahydronaphthalene: 2a, 2c and 2d) and cationic [Ru(η6-arene)Cl(Ph2P(CH2)3SPh-κP,κS)]X complexes (arene = mesitylene, 1,4-dihydronaphthalene; X = Cl: 3b, 3e; arene = benzene, mesitylene, indane, 1,2,3,4-tetrahydronaphthalene, and 1,4-dihydronaphthalene; X = PF6: 4a–4e) complexes were prepared and characterized by elemental analysis, IR, 1H, 13C and 31P NMR spectroscopy and also by single-crystal X-ray diffraction an...
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