- Characterization of the effects of aryl-azido compounds and UVA irradiation on the viral proteins and infectivity of human immunodeficiency virus type 1
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Hydrophobic UV-activatable compounds have been shown to partition into the hydrophobic region of biological membranes to selectively label transmembrane proteins, and to inactivate enveloped viruses. Here, we analyze various UV-activatable azido- and iodo-based hydrophobic compounds for their ability to inactivate a model-enveloped virus, human immunodeficiency virus (HIV-1 MN). Treatment of HIV-1 with 1,5-diazidonapthalene (DAN), 1-iodo, 5-azidonaphthalene (INA), 1-azidonaphthalene (AzNAP) or 4,4′-diazidobiphenyl (DABIPH) followed by UVA irradiation for 2 min resulted in complete viral inactivation, whereas treatment using analogous non-azido-containing controls had no effect. Incorporation of an azido moiety within these hydrophobic compounds to promote photoinduced covalent reactions with proteins was found to be the primary mechanism of viral inactivation for this class of compounds. Prolonged UVA irradiation of the virus in the presence of these azido compounds resulted in further modifications of viral proteins, due to the generation of reactive oxygen species, leading to aggregation as visualized via Western blot analysis, providing additional viral modifications that may inhibit viral infectivity. Furthermore, inactivation using these compounds resulted in the preservation of surface antigenic structures (recognized by neutralizing antibodies b12, 2g12 and 4e10), which is favorable for the creation of vaccines from these inactivated virus preparations.
- Belanger, Julie M.,Raviv, Yossef,Viard, Mathias,Jason De La Cruz, Michael,Nagashima, Kunio,Blumenthal, Robert
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- Synthesis of a novel series of 1,2,3-triazole-containing artemisinin dimers with potent anticancer activity involving Huisgen 1,3-dipolar cycloaddition reaction
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A series of C-10 acetal triazolylartemisinin dimers were prepared via the Huisgen 1,3-dipolar cylcoaddition of artemisinin-derived terminal alkynes with 10-azidoartemisinin and various aliphatic and aromatic diazides. All the artemisinin dimers synthesized exhibited strong growth inhibition activity against several cancer cell lines. Georg Thieme Verlag Stuttgart New York.
- Saikia, Bishwajit,Saikia, Partha Pratim,Goswami, Abhishek,Barua, Nabin C.,Saxena, Ajit K.,Suri, Nitasha
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- Linear C2 symmetric compound, lanthanide polynuclear complex and preparation method and application of lanthanide polynuclear complex
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The invention discloses a linear C2 symmetric compound, a lanthanide polynuclear complex and a preparation method and application of the lanthanide polynuclear complex, and belongs to the field of photochemical supramolecules. The structural formula of the linear C2 symmetric compound is shown in the specification. The linear C2 symmetric compound is obtained by carrying out triazole cyclization reaction on an azide compound and an alkyne compound at the temperature of 50-70 DEG C. The lanthanide polynuclear complex has a general formula Ln2nL3n, wherein Ln is selected from lanthanide, L is anorganic ligand selected from the linear C2 symmetric compound, and n is selected from 1 or 2. The preparation method comprises the steps: carrying out a reaction on a lanthanide Ln precursor with theorganic ligand L at the temperature of 30-50 DEG C. The linear C2 symmetric compound comprises a triazole-pyridine-amide chelating group, can improve the efficiency of energy transfer from an intermediate chromophore of the ligand to a rare earth center, and improve the construction of a lanthanide complex having a high nuclear number, and thus the obtained complex having strong light-emitting properties and includes a lanthanide organic polyhedral cage having a high nuclear number.
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Paragraph 0112; 0123-0124
(2020/08/18)
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- 1,2,3-TRIAZOLE CONTAINING ARTEMISININ COMPOUNDS AND PROCESS FOR PREPARATION THEREOF
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The present invention relates to 1,2,3-triazole containing artemisinin compounds and process for preparation thereof. Described herein is the synthesis, bioassay results and usefulness of the artemisinin derived compounds resulting from 1,3-di-polar cycloaddition reaction of artemisinin derived azide or alkyne with aliphatic or aromatic diazides. These 1,2,3-triazole containing artemisinin derived compounds embodied in this document are found to be active against various cancer cell-lines.
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Paragraph 0063; 0080; 0081; 0082
(2014/01/08)
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- Synthesis and self-assembly of tetraphenylethene and biphenyl based AIE-active triazoles
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Self-assembly of fluorescent functional materials has attracted increasing interest in the fabrication of optoelectronic and biological nanodevices. Tetraphenylethene (TPE) is a typical dye molecule with aggregation-induced- emission (AIE) characteristics. Melding TPE carrying triple-bond functionality with diazide-containing biphenyl through "click" chemistry generates AIE-active luminogens [1,1′-biphenyl]-4,4′-diyl bis(6-(4-(4-(1,2,2- triphenylvinyl)phenyl)-1H-1,2,3-triazol-1-yl) hexanoate) [1(5)] and [1,1′-biphenyl]-4,4′-diyl bis(11-(4-(4-(1,2,2-triphenylvinyl)phenyl) -1H-1,2,3-triazol-1-yl) undecanoate) [1(10)] with solid state efficiencies up to unity. Slow addition of dilute THF solutions of 1(m) (m = 5, 10) into nonsolvents such as n-hexane and water yields self-assembled white wooly solids. TEM and SEM observations reveal the (helical) nanofibrous structure of the aggregates. Upon cooling from their concentrated hot solutions, 1(m) readily precipitate. Meanwhile, they can also form gels at high concentrations. Both precipitates and gels of 1(m) exhibit structures similar to those of the aggregates formed in nonsolvents. These results indicate that 1(m) can facilely self-assemble into high emission efficiency (helical) nanofibers, thus paving the way for their optoelectronic and biological applications. The Royal Society of Chemistry 2012.
- Yuan, Wang Zhang,Mahtab, Faisal,Gong, Yongyang,Yu, Zhen-Qiang,Lu, Ping,Tang, Youhong,Lam, Jacky W. Y.,Zhu, Caizhen,Tang, Ben Zhong
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supporting information; experimental part
p. 10472 - 10479
(2012/08/13)
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- Photochemical reactions of nitroso oxides at low temperatures: The first experimental evidence for dioxaziridines
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Several singlet nitroso oxides (3a - e) were generated by the thermal reaction of triplet nitrenes (2a - e) with triplet oxygen at 95 K in 2-methyltetrahydrofuran. After photolysis of the nitroso oxides at 77 K using strong light intensities, the formation of intermediates was observed for the first time. From spectroscopic, kinetic, and chemical arguments, we postulate the formation of the following dioxaziridines: 4-(dioxaziridinyl)stilbene (4a), 4-(dioxaziridin-yl)-4′-nitrostilbene (4b), 4′-(dioxaziridin-yl)-4-(dimethylamino)stilbene (4c), 4′-(dioxaziridin-yl)-4-aminobiphenyl (4d), and 4-(dioxaziridin-yl)-4′-(nitrene-substituted)stilbene (4f). All dioxaziridines observed are highly reactive species. At 77 K, they react thermally to form the corresponding nitro compounds (5). The velocity of the ring opening reaction of the dioxaziridines (4 → 5) is not significantly influenced by substituents; the rate constants at 77 K are all equal to 0.0030 ± 0.0005 s-1. The transients were characterized by stationary UV/vis and/or ESR spectroscopy. Ab initio calculations of the thermal reaction of the nonsubstituted dioxaziridine (6) and N-phenyldioxaziridine (9) were performed. From this, it follows that dioxaziridines are experimentally observable species which are separated from the corresponding nitro products by an orbital symmetry-forbidden barrier.
- Harder,Wessig,Bendig,Stoesser
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p. 6580 - 6588
(2007/10/03)
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- Models for intramolecular exchange in organic π-conjugated open-shell systems: A comparison of three non-kekule biphenyldinitrenes
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The important effect of connectivity upon the nature of intramolecular exchange coupling of unpaired electrons by the biphenyl group was investigated by cryogenic matrix photolysis of diazide precursors expected to yield biphenyl-3,4′-dinitrene (1), biphenyl-3,3′-dinitrene (2), and biphenyl-4,4′-dinitrene (3). System 1 was predicted by parity-based qualitative models to exhibit a high-spin ground state. By Curie law analysis of its electron spin resonance (ESR) spectrum at cryogenic temperatures in frozen 2-methyltetrahydrofuran solution, 1 was found to be a quintet ground-state dinitrene with zero field splitting (zfs) parameters of |D/hc| = 0.153 cm-1, |E/hc| = 0.003 cm-1. System 2 was predicted to be disjoint with nearly-degenerate high-spin and low-spin states. Cryogenic frozen solution ESR spectroscopy showed no ESR-active dinitrene 2 upon extended photolysis of its appropriate diazide precursor, although the related mononitrene with zfs of |D/hc| = 0.996 cm-1 was clearly visible. We presume that system 2 was produced in this experiment, but that it acts either as a singlet ground-state dinitrene or as a pair of isolated mononitrenes. A biradical ESR spectrum was found for photolysis of the diazide precursor to 3, with zfs of |D/hc| = 0.189 cm-1 and |E/hc| -1. The thermal dependence of this biradical spectrum shows it to be an excited state, consistent with quinonoidal dinitrene 3 having a singlet ground state and a triplet excited state ca. 0.6 kcal/mol higher in energy. The results for dinitrenes 1-3 were compared to related work on dicarbene molecules described by others, and it was found that the dinitrenes and dicarbenes exhibit similar electron exchange coupling behavior.
- Minato, Masaki,Lahti, Paul M.,Van Willigen, Hans
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p. 4532 - 4539
(2007/10/02)
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- Amyloidosis and Alzheimer's disease diagnostic assay and reagents therefor
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The presence and location of amyloid deposits in an organ or body area of a patient is effected by intravenous administration of novel radioactive iodine-labeled amyloid binding compounds and preferably 123 I-labeled compounds to the patient an
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- Zum Substituenteneinfluss auf die UV-VIS-spektroskopischen Eigenschaften von Mono- und Bisaziden
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The UV-VIS spectroscopic properties of three substituted 2,6-bis--cyclohexanone, 17 substituted p-azidobenzalacetophenone and three substituted p,p'-diazidobiphenyls are reported.The influence of the substituents can be described
- Sauer, E.,Schopf, G.,Czarnetzki, K.,Bendig, J.
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p. 1185 - 1195
(2007/10/02)
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