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Compound 1, 2-(4-phenoxyphenylsulfonylmethyl)thiirane, is a potent and selective inhibitor for human gelatinases (J. Am. Chem. Soc. 2000, 122, 6799-6800), enzymes implicated in a number of diseases, including cancer. This compound is showing excellent promise in animal trials in a number of disease models. Large quantities of this compound were necessary for these studies. A convenient four-step synthetic route for compound 1 is described herein. The synthesis is amenable to scale-up to tens of grams and gives an overall yield of 57% for this important compound. 相似文献
3.
Birck C Cha JY Cross J Schulze-Briese C Meroueh SO Schlegel HB Mobashery S Samama JP 《Journal of the American Chemical Society》2004,126(43):13945-13947
4.
The growth ofBacillus amyloliquefaciens in the aqueous two-phase system, made up of polyethylene glycol, dextran, and water, was investigated. Generally,Bacillus partitions in the dextran phase, but the magnitude of the separation depends largely on the overall composition of polymers
in the phase system. The kinetics of growth ofBacillus amyloliquefaciens was studied in the polyethylene glycol-rich continuous phase, dextran-rich dispersed phase, and in the mixed phase. From
the kinetic data it appears that increasing the overall polymer composition causes the cells to adsorp at the interface. On
the other hand, partition measurements indicate that increasing polymer concentrations make the cell partitioning more one-sided.
This anomaly is explained by studying the interfacial adsorption of cells via dynamic surface tension measurements. 相似文献
5.
Headspace solvent microextraction A new method applied to the preconcentration of 2-butoxyethanol from aqueous solutions into a single microdrop 总被引:1,自引:0,他引:1
A new procedure and experimental setup for the headspace solvent microextraction of volatile organic materials from aqueous sample solutions is described. The extraction occurs by suspending a 3-μl drop of the solvent from the tip of a microsyringe to the headspace of a stirred aqueous sample solution for a preset extraction time. The temperature of the microdrop and the bulk of sample solution should be kept constant at optimized values. The sample analyses were carried out by gas chromatography. The procedure was successfully applied to the extraction and determination of 2-butoxyethanol from content of some color samples used for painting the outer coverage of some machines such as coolers, refrigerator, cloths machine, etc. Parameters such as extraction time, nature of extraction solvent, size of microdrop, sample volume, stirring rate, ionic strength and pH of sample solution were studied and optimized, and the method performance was evaluated. 相似文献
6.
Ikejiri M Bernardo MM Meroueh SO Brown S Chang M Fridman R Mobashery S 《The Journal of organic chemistry》2005,70(14):5709-5712
[structure: see text] Matrix metalloproteinases (MMPs), of which 26 are known, have been implicated in a number of pathological conditions, including tumor metastasis. We have previously described the first mechanism-based inhibitor for MMPs (J. Am. Chem. Soc. 2000, 122, 6799-6800), which in chemistry mediated by the active site zinc ion selectively and covalently inhibits MMP-2, -3, and -9. Computational analyses indicated that this selectivity in inhibition of MMPs could be improved by design of new variants of the inhibitor class. We report herein the syntheses of methyl 2-(4-{4-[(2-thiiranylpropyl)sulfonyl]phenoxy}phenyl)acetate (3) and 2-(4-{4-[(2-thiiranylpropyl)sulfonyl]phenoxy}phenyl)acetic acid (4), and show that compound 3 serves as a mechanism-based inhibitor exclusively for MMP-2. This molecule should prove useful in delineating the functions of MMP-2 in biological systems. 相似文献
7.
Synergetic catalytic effect of rGO,Pd, Fe3O4 and PPy as a magnetically separable and recyclable nanocomposite for coupling reactions in green media 下载免费PDF全文
In this paper, rGO/Pd–Fe3O4@PPy as an efficient stable nanocomposite was synthesized. To understand the synergetic effects of rGO, Pd, Fe3O4 and PolyPyrrole, the performance of rGO/Pd–Fe3O4@PPy as a heterogeneous recyclable nanocatalyst in the green synthesis of C‐C and C‐O coupling products, as well as different conditions are studied. Synthesized rGO/Pd–Fe3O4@PPy was characterized by FT‐IR, XRD, FE‐SEM, EDS, TGA and AFM analysis. Best results are obtained under sonication in H2O for C‐C coupling and by ball‐milling for C‐O coupling. The benefits of this method include: green solvents and conditions, absence of external base, low reaction times with high yield and easy work‐up method. 相似文献
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Nosrati Sahar Molavipordanjani Sajjad Emami Saeed Abedi Seyed Mohammad Talebpour Amiri Fereshteh Hosseinimehr Seyed Jalal 《Journal of Radioanalytical and Nuclear Chemistry》2020,323(1):205-211
This study presents [99mTc]BPTG-1 and [99mTc]BPTG-2 for glioblastoma imaging. In vitro cellular uptakes of these radiotracers were examined in SKOV-3, MCF-7, U87-MG, HT-29, and A549 cell lines. U87-MG cell line displayed the highest radiotracers uptakes. Biodistribution study in U87-MG tumor bearing mice revealed higher uptake of radiotracers in tumor than muscle and brain. Liver, intestine, and kidneys displayed the highest radioactivity uptakes. The main route of radiotracers elimination was hepatobiliary. Due to the brain uptake of these radiotracers, they are promising radiotracers for future studies in the diagnosis of glioblastoma.
相似文献