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1.
Roger Alberto 《Journal of organometallic chemistry》2007,692(6):1179-1186
This article will emphasize the particular role of organometallic radiopharmaceutical chemistry, namely the need for syntheses from water and the emerging implications for other (bio)organometallic fields. After some basic insights into the different directions of bioorganometallic chemistry, some facets of the [M(CO)3]+ (M = Tc, Re) moiety are reviewed and discussed in the respective context. The mechanism for the synthesis of [M(OH2)3(CO)3]+ which is still little understood, will be touched. The formation of additional M-C bonds is exemplified with cyclopentadienyl chemistry, the potential impact on targeted molecular imaging with the labelling of amino acids and the reactivity towards essential biomolecules such as guanine is shown. Future perspectives and implications for organometallic radiopharmaceutical chemistry will close this article. 相似文献
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Johannes ZagermannAnthony Deally Nils Metzler-NolteHelge Müller-Bunz Denise WallisMatthias Tacke 《Polyhedron》2011,30(14):2387-2390
An alkyne-substituted fulvene was transformed via hydridolithiation followed by transmetallation with titanium tetrachloride into bis-[p-(prop-2-ynyloxy)-benzyl-cyclopentadienyl] titanium(IV) dichloride. Single crystals of this titanocene derivative could be obtained and the structure determined by X-ray diffraction. It showed that this compound crystallises in the space group C2/c with four molecules in the monoclinic cell. The alkyne-substituted titanocene dichloride derivative was then subject to a copper-catalysed azide-alkyne cycloaddition with its azide-functionalised methylester-protected phenylalanine reaction partner in order to form a linking triazole. This reaction was performed under anhydrous conditions employing a dichloromethane/acetonitrile solvent mixture with copper(I) iodide and 2,6-lutidine as the catalyst system. Under these conditions the adduct between the protein mimic and the titanocene was formed without hydrolysing the titanium dichloride moiety. 相似文献
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Ferreiro-Vera C Ribeiro JP Mata-Granados JM Priego-Capote F Luque de Castro MD 《Journal of chromatography. A》2011,1218(38):6720-6726
Standard operating procedures (SOPs) are of paramount importance in the analytical field to ensure the reproducibility of the results obtained among laboratories. SOPs gain special interest when the aim is the analysis of potentially unstable compounds. An SOP for analysis of lipid hydroperoxides (HpETEs) is here reported after optimization of the critical steps to be considered in their analysis in human serum from sampling to final analysis. The method is based on automated hyphenation between solid-phase extraction (SPE) and liquid chromatography-mass spectrometry (LC-MS). The developed research involves: (i) optimization of the SPE and LC-MS steps with a proper synchronization; (ii) validation of the method-viz. accuracy study (estimated as 86.4% as minimum value), evaluation of sensitivity and precision, which ranged from 2.5 to 7.0 ng/mL (0.25-0.70 ng on column) as quantification limit and precision below 13.2%), and robustness study (reusability of the cartridge for 5 times without affecting the accuracy and precision of the method); (iii) stability study, involving freeze-thaw stability, short-term and long-term stability and stock solution stability tests. The results thus obtained allow minimizing both random and systematic variation of the metabolic profiles of the target compounds by correct application of the established protocol. 相似文献
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Dr. Jiakang Tang Dr. Ji Liu Dr. Qizhen Zheng Rui Yao Prof. Dr. Ming Wang 《Angewandte Chemie (International ed. in English)》2023,62(48):e202312784
Mitochondria-targeted bioorthogonal catalysis holds promise for controlling cell function precisely, yet achieving selective and efficient chemical reactions within organelles is challenging. In this study, we introduce a new strategy using protein-integrated hydrogen-bonded organic frameworks (HOFs) to enable synergistic bioorthogonal chemical catalysis and enzymatic catalysis within mitochondria. Utilizing catalytically active tris(4,4′-dicarboxylicacid-2,2′-bipyridyl) ruthenium(II) to self-assemble with [1,1′-biphenyl]-4,4′-biscarboximidamide, we synthesized nanoscale RuB-HOFs that exhibit high photocatalytic reduction activity. Notably, RuB-HOFs efficiently enter cells and preferentially localize to mitochondria, where they facilitate bioorthogonal photoreduction reactions. Moreover, we show that RuB-HOFs encapsulating catalase can produce hydrogen sulfide (H2S) in mitochondria through photocatalytic reduction of pro-H2S and degrade hydrogen peroxide through enzymatic catalysis simultaneously, offering a significant neuroprotective effect against oxidative stress. Our findings not only introduce a versatile chemical toolset for mitochondria-targeted bioorthogonal catalysis for prodrug activation but also pave the way for potential therapeutic applications in treating diseases related to cellular oxidative stress. 相似文献
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靶向抗肿瘤药物甲氨喋呤-琥珀酰壳聚糖缀合物的制备及其体外稳定性的初步探讨 总被引:7,自引:1,他引:6
报道了甲氨喋呤-琥珀酰壳聚糖缀合物的合成方法,并通过紫外光谱、红外光谱及核磁共振谱进行了结构验证.流式细胞仪的检测结果表明,N-琥珀酰壳聚糖对K562白血病肿瘤细胞具有较强的亲和性;溶解性实验结果表明,甲氨喋呤-琥珀酰壳聚糖缀合物的水溶性较好(pH=1~14);体外释放实验结果表明,缀合物性质稳定,能明显延缓甲氨喋呤的释放,为抗肿瘤药物的靶向及缓控释给药体系的研究提供了初步参考. 相似文献
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Qing Lin Jiang Li Hai Lei Chen Jiao Lu Zhi Rong Zhang Yong Wu 《中国化学快报》2008,19(2):127-129
A novel bifunctional glycolipid which carded a cluster of thiogalactosides as the hepatocyte targeting ligand for gene delivery was prepared. Hexa-antennary alcohol 1 was used as the core scaffold to attach a cholesterol molecule by a poly(ethylene glycol) chain, while its remaining branches were linked with five acetylgalactosides, which would be deacetylated later to produce pentaantennary galactoside. Liposome containing the galactoside showed high affinity and transfection activity in hepatoma cells HepG2. 相似文献
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Lei Tang Yong Wu Jiao Lu Zhi Rong Zhang Jin Cheng Yang Li Hai 《中国化学快报》2007,18(5):513-515
A novel bifunctional compound carrying cluster thiogalactoside as the cell targeting ligands was synthesized for gene delivery to hepatocytes. Tetra-antennary dendr-OMs4 5 was used as a scaffold for the attachment of three galactosides, while the other mesylate end was linked with cholesterol through poly(ethylene glycol) chain. This design provided an effective entry for the synthesis of the bifunctional compound. 相似文献
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《Arabian Journal of Chemistry》2022,15(3):103672
Porous nanosized metal–organic frameworks (MOFs) are becoming possible candidates as drug-delivery nanocarriers for their versatile porous structures and large loadings of drugs. However, controlling synthesis of MOFs with uniform morphology, good biocompatibility and targeting drug delivery is still a challenge, which greatly limits their clinical applications. Herein, a multifunctional nano-sized drug-delivery material MIL-101(Fe)@FU@FA with a uniform particle size about 500 nm was successfully synthesized for targeting therapeutic purposes. The targeting reagent folic acid (FA) molecules are connected on the surface of 5-FU-loaded nanoparticle MIL-101(Fe)-NH2 by a covalent conjugation. Cytotoxicity tests showed that the synthesized nanoparticles are biocompatible and can significantly inhibit cell proliferation on SMMC-7721 cells compared with MIL-101(Fe)@FU and free 5-FU. The cell metastasis and invasion experiments proved that the nanoparticles had a good anti-metastasis ability to tumor cells. Mechanistically, MIL-101(Fe)@FU@FA induces apoptosis of SMMC-7721 cells and block cell cycle progression in the G2/M phase. Taken together, the drug-loaded nanoparticles MIL-101(Fe)@FU@FA have the effect of targeting and sustained release to achieve the therapeutic effect. 相似文献
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Multifunctional nanocarriers with multilayer core-shell architecture were prepared by coating superparamagnetic Fe3O4 nanoparticles with diblock copolymer folate-poly(ethylene glycol)-b-poly(glycerol monomethacrylate) (FA-PEG-b- PGMA), and triblock copolymer methoxy poly(ethylene glycol)-b-poly(2-(dimethylamino) ethyl methacrylate)-b- poly(glycerol monomethacrylate) (MPEG-b-PDMA-b-PGMA). The PGMA segment was attached to the surfaces of Fe304 nanoparticles, and the outer PEG shell imparted biocompatibility. In addition, folate was conjugated onto the surfaces of the nanocarriers. Cisplatin was then loaded into the nanocarrier by coordination between the Pt atom in cisplatin and the amine groups in the inner shell of the multilayer architecture. The loaded cisplatin showed pH-responsive release: slower release at pH 7.4 (i.e. mimicking the blood environment) and faster release at more acidic pH (i.e. mimicking endosome/lysosome conditions). All of the cisplatin-loaded nanoparticles showed concentration-dependent cytotoxicity in HeLa cells. However, the folate-conjugated cisplatin-loaded carriers exhibited higher cytotoxicity in HeLa cells than non-folate conjugated cisplatin-loaded carriers. 相似文献