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1.
The alkaloids salsolidine, salsoline and (R)-N-benzyl-l-phenylethylamine were added to 7-methyl-2-isobornylphenol using an aminomethylation reaction.
Translated from Khimiya Prirodnykh Soedinenii, No. 4, pp. 367–368, July–August, 2008. 相似文献
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A series of chlorins containing a vinyl group on the periphery of the chlorin ring that was attached by linkers of various
length, potential monomers for synthesis of polymers containing chlorin via copolymerization, was synthesized from methylpheophorbide
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Translated from Khimiya Prirodnykh Soedinenii, No. 2, pp. 163–166, March–April, 2007. 相似文献
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Grin M. A. Titeev R. A. Brittal D. I. Chestnova A. V. Feofanov A. V. Lobanova I. A. Sivaev I. B. Bregadze V. I. Mironov A. F. 《Russian Chemical Bulletin》2010,59(1):219-224
Novel boron-containing conjugates based on the alkynylated cobalt bis(dicarbollide) anion and chlorin e
6 and purpurinimide p-iodophenyl derivatives were synthesized by the Sonogashira reaction. These conjugates can accumulate in the cancer cell cytoplasm
and can be considered as potential candidates for using in boron neutron capture therapy of tumors. 相似文献
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Abraham J. Domb Galina Linden Itzhack Polacheck Simon Benita 《Journal of polymer science. Part A, Polymer chemistry》1996,34(7):1229-1236
The coupling of nystatin (Nys), a water-insoluble antifungal agent, to dextran via an imine or amine bond was systematically investigated. Dextran was first oxidized to dialdehyde dextran using potassium periodate, purified from the oxidizing agent, and reacted with Nys to form the Schiff base. The Schiff base was reduced to the amine using borohydride. All reactions took place in water. The purification of the oxidized dextran from the oxidizing agent was essential to prevent oxidative degradation of Nys at the coupling step. The effects on the coupling yield of the following factors: dextran molecular weight, degree of oxidation (aldehyde content), Nys to dextran ratio, temperature, and reaction pH were studied. A 95% coupling yield was obtained at the optimized coupling conditions: pH 8.9 ± 0.1, 50% degree of oxidation, and initial ratio of Nys to dialdehyde dextran 1:2.5. In all experiments, dextran was decreased in molecular weight during the oxidation step. Both imine and amine forms of Nys-dextran conjugates were soluble in water and exhibited improved stability in aqueous solutions as compared to the unbound drug. The conjugates showed comparable minimum inhibitory concentration (MIC) values against Candida albicans and Cryptococcus neoformans. The conjugates were about 25 times less toxic than free Nys after a single injection in mice. © 1996 John Wiley & Sons, Inc. 相似文献
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Macrolide-nucleoside and macrolide-nucleobase conjugates (chimeras) have been synthesised by linking erythromycin A oxime derivatives and clarithromycin C11,C12-oxazolidinone derivatives with 3′-amino-3′-deoxythymidine or adenine through different spacers; clarithromycin-adenine conjugate 16a is the most active species against Micrococcus luteus. 相似文献
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I. Yu. Chukicheva O. V. Sukrusheva A. V. Kutchin 《Russian Journal of Organic Chemistry》2017,53(4):520-524
4-(3-Sulfanylpropyl)-2-isobornyl-6-methylphenol and 4-(sulfanylmethyl)-2,6-diisobornylphenol were synthesized from the corresponding 4-(bromoalkyl)phenols according to known procedures. Isobornylphenol with a trimethylene linker was converted into thiol by alkaline hydrolysis of thiouronium salt. The methylene-bridged analog was obtained by reduction of S-benzyl thioacetate with LiAlH4. 相似文献
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Arturo Battaglia Andrea Guerrini Greta Varchi Ezio Bombardelli 《Tetrahedron letters》2006,47(16):2667-2670
Efficient syntheses of two taxol analogs bearing the linear polyamine spermine at 7- and 10-positions of paclitaxel and 10-deacetyl-paclitaxel have been developed. These polyamine-taxol-conjugates were isolated as water soluble difluoride salts. The aim of the present work was to introduce a chemical modification into taxol skeleton in order to increase drug selectivity toward tumor cells. The cytotoxic activity of these conjugates was evaluated in MCF7 and MCF7-R cell lines. The observed low cytotoxicity suggests that these conjugates could act as potential prodrugs. 相似文献
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Khudyaeva I. S. Belykh D. V. Shevchenko O. G. Maximova M. A. Zainullina L. F. Vakhitova Yu. V. Shchukina O. V. Buravlev E. V. Chukicheva I. Yu. Kutchina A. V. 《Russian Chemical Bulletin》2017,66(11):2157-2164
Russian Chemical Bulletin - Conjugates containing chlorine and isobornylphenolic fragments, which are connected by spacers of different lengths, were synthesized from methyl pheophorbide a. The... 相似文献
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Monomer conjugation of an enzyme followed by copolymerization with free monomer is a useful method of enzyme immobilization.
L-asparaginase was conjugated with N-succinimidyl acrylate. Analysis of the conjugated enzyme via isoelectric focusing showed
that a molar ratio of 9.5 free monomers per enzyme was needed during the conjunction for each vinyl group bound. Only 3% of
the enzyme activity was lost per vinyl group added, and conjugation of an average of four monomers per enzyme thermally destabilized
the enzyme only at temperatures above 50‡C. Activity of the enzyme at physiological temperatures was relatively unaffected. 相似文献
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I. Yu. Chukicheva O. V. Sukrusheva L. I. Mazaletskaya A. V. Kuchin 《Russian Journal of General Chemistry》2016,86(10):2325-2331
Alkylation of isobornylphenols with allylbenzene in the presence of homogeneous and heterogeneous catalysts of different nature has been studied. The maximum yield of phenols containing isobornyl and 1-phenylpropyl moieties has been achieved in the presence of catalyst FIBAN K-1 at 100°С and catalyst concentration of 10%. The inhibiting action of isobornylphenol derivatives has been studied in the model reaction of ethylbenzene oxidation. Hybrid antioxidants on the basis of isobornylphenols were found to actively interact with peroxide radicals and, therefore, they can be considered as promising additives for conservation of quality and increase in service life of different organic compounds and materials. 相似文献
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Literature data on the alkylation of phenolic compounds by mono-, sesqui-, and diterpenes in the presence of various catalysts are reviewed.Novosibirsk Institute of Organic Chemistry, Siberian Division, Russian Academy of Sciences, Novosibirsk, fax (3832) 34 47 52, e-mail: shreed@nioch.nsc.ru. Translated from Khimiya Prirodnykh Soedinenii, No. 3, pp. 198–207, May–June, 2000. 相似文献
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A general approach towards the preparation of peptide-steroid conjugates has been addressed. Utilizing the Ugi reaction, five peptidomimetic-steroid hybrids were achieved in good to excellent yields from carboxy- and amino-spirostanes and mono-protected α-amino acids. Diverse synthetic routes, specially focused on the formation of secosteroids, were implemented to introduce Ugi-type functionalities at different positions of the steroidal nucleus. This versatile approach is suitable for the formation of stable conjugates of steroids with other biologically relevant molecules. 相似文献
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Jennifer A. Loch Cornelia Borgmann Robert H. Crabtree 《Journal of molecular catalysis. A, Chemical》2001,170(1-2):75-80
New syntheses of PEG-(OCH2C5H4N)2 and PEG-(OC6H4PPh2)2 (PEG: poly(ethylene glycol)) conjugates are reported. An iridium hydrogenation catalyst 1, is shown to catalyze hydrogenation in a water/substrate two-phase system. Attachment of 1 to PEG to make 2 and 3 succeeds in making the complex water-soluble and allows it to retain some of its catalytic ability, but leads to micelle formation that inhibits the separation of organic and aqueous phases. 相似文献
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Polymer therapeutics is a very promising and rapidly growing area of nanomedicine, which has significantly improved the therapeutic potential of low‐molecular‐weight drugs and proteins for cancer treatment. Conjugation of toxic drugs to high‐molecular‐weight carriers can lead to reduction in systemic toxicity, longer retention time in the body, improved biodistribution and therapeutic efficacy, and site‐specific passive accumulation thanks to the leaky tumor vasculature. Furthermore, a targeting moiety can be coupled to the polymer–drug conjugate in order to actively and selectively deliver it to the desired tissue and cellular target. This review presents a summary of currently developed polymer therapeutics with detailed focus on their components and supramolecular structure. The use of polymeric nanocarriers for cancer angiogenesis‐targeted delivery is illustrated by specific examples. Copyright © 2013 John Wiley & Sons, Ltd. 相似文献