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Downstream modification of piperazin-2-ones obtained by the Castagnoli-Cushman reaction leads to a novel version of the medicinally relevant 1,2,5-benzothiadiazepin-4-one-1,1-dioxide scaffold. The relative stereochemistry remained trans as evidenced by the spectroscopic data and the single-crystal X-ray analysis. 相似文献
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Liubov V. Sokolenko Yurii L. Yagupolskii Liliia S. Kumanetska Jérôme Marrot Emmanuel Magnier Volodimir O. Lipetskij Ihor V. Kalinin 《Tetrahedron letters》2017,58(13):1308-1311
Methyl 3-(dimethylamino) acrylates containing trifluoromethylsulfenyl-, trifluoromethylsulfinyl-, and trifluoromethylsulfonyl groups were synthesized and their utility demonstrated by reactions with aliphatic and aromatic amidines to produce 2,5-substituted 4(3H)-pyrimidones. Cyclization reactions of enaminones with urea or thiourea led to 5-substituted uracil or 2-thiouracil derivatives, respectively. 相似文献
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I. Kraicheva E. Vodenicharova B. Shivachev R. Nikolova A. Kril M. Topashka-Ancheva 《Phosphorus, sulfur, and silicon and the related elements》2013,188(11):1535-1547
Abstract The X-ray crystal structures of the anthracene-derived bis-aminophosphonates 4.4′-bis[N-methyl(diethoxyphosphonyl)-1-(9-anthryl)]diaminodiphenylmethane (1) and 1,3-bis [N-methyl(diethoxyphosphonyl)-1-(9-anthryl)]diaminobenzene (3) are reported. The X-ray analyses demonstrated that both compounds crystallize in a centrosymmetric manner containing a meso-form (1) and a pair of enantiomers (3). The cytotoxic potential, genotoxicity, and antiproliferative activity of bis-aminophosphonates 1 and bis[N-methyl(diethoxyphosphonyl)-1-(9-anthryl)]benzidine (2), as well as their subcellular distribution in a tumor cell culture system, are also discussed. Compounds 1 and 2 showed optimal antiproliferative activity to human tumor cells from colon carcinoma line HT-29. In vitro and in vivo safety testing revealed that the compounds exert lower toxicity to normal cells as compared with well-known anticancer and cytotoxic agents. Supplemental materials are available for this article. Go to the publisher's online edition ofPhosphorus, Sulfur, and Silicon and the Related Elementsto view the free supplemental file. 相似文献
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Yafarova Liliia V. Silyukov Oleg I. Myshkovskaya Tatiana D. Minich Iana A. Zvereva Irina A. 《Journal of Thermal Analysis and Calorimetry》2021,143(1):87-93
Journal of Thermal Analysis and Calorimetry - Protonation and hydration processes of layered perovskite-like oxide KCa2Nb3O10 during the reaction with nitric acid solutions with different... 相似文献
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Kasian Natalia Vashchenko Olga Budianska Liliia Brodskii Roman Lisetski Longin 《Journal of Thermal Analysis and Calorimetry》2019,136(2):795-801
Journal of Thermal Analysis and Calorimetry - Phase transitions of multibilayer structures of hydrated L-α-dipalmitoyl- and L-α-dimyristoylphosphatidylcholine (DPPC and DMPC) were studied... 相似文献
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Neli Christova Boryana Tuleva Anton Kril Milka Georgieva Spiro Konstantinov Ivan Terziyski Biliana Nikolova Ivanka Stoineva 《Applied biochemistry and biotechnology》2013,170(3):676-689
A newly isolated indigenous strain BN10 identified as Pseudomonas aeruginosa was found to produce glycolipid (i.e., rhamnolipid-type) biosurfactants. Two representative rhamnolipidic fractions, RL-1 and RL-2, were separated on silica gel columns and their chemical structure was elucidated by a combination of nuclear magnetic resonance and mass spectroscopy. Subsequently, their cytotoxic effect on cancer cell lines HL-60, BV-173, SKW-3, and JMSU-1 was investigated. RL-1 was superior in terms of potency, causing 50 % inhibition of cellular viability at lower concentrations, as compared to RL-2. Furthermore, the results from fluorescent staining analysis demonstrated that RL-1 inhibited proliferation of BV-173 pre-B human leukemia cells by induction of apoptotic cell death. These findings suggest that RL-1 could be of potential for application in biomedicine as a new and promising therapeutic agent. 相似文献
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Rashmi Mahajan Mona Rouhi Sudhirkumar Shinde Thomas Bedwell Anil Incel Liliia Mavliutova Sergey Piletsky Ian A. Nicholls Brje Sellergren 《Angewandte Chemie (Weinheim an der Bergstrasse, Germany)》2019,131(3):737-740
We report an approach integrating the synthesis of protein‐imprinted nanogels (“plastic antibodies”) with a highly sensitive assay employing templates attached to magnetic carriers. The enzymes trypsin and pepsin were immobilized on amino‐functionalized solgel‐coated magnetic nanoparticles (magNPs). Lightly crosslinked fluorescently doped polyacrylamide nanogels were subsequently produced by high‐dilution polymerization of monomers in the presence of the magNPs. The nanogels were characterised by a novel competitive fluorescence assay employing identical protein‐conjugated nanoparticles as ligands to reversibly immobilize the corresponding nanogels. Both nanogels exhibited Kd<10 pM for their respective target protein and low cross‐reactivity with five reference proteins. This agrees with affinities reported for solid‐phase‐synthesized nanogels prepared using low‐surface‐area glass‐bead supports. This approach simplifies the development and production of plastic antibodies and offers direct access to a practical bioassay. 相似文献
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