- Enzymatic incorporation of an antibody-activated blue fluorophore into DNA
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(Chemical Equation Presented) Antibodies as light switches: The deoxy-nucleotide analogue-stilbene conjugate 1 can be incorporated into nascent DNA by DNA polymerase activity. The blue fluorescence of stilbene is detected only upon binding of an antibody
- Kaufmann, Gunnar F.,Meijler, Michael M.,Sun, Chengzao,Chen, Da-Wei,Kujawa, David P.,Mee, Jenny M.,Hoffman, Timothy Z.,Wirsching, Peter,Lerner, Richard A.,Janda, Kim D.
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Read Online
- Synthesis and characterization of a new polymer support for a metallocene catalyst
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The synthesis of a novel polymer support and its use for the attachment of a metallocene catalyst is described in detail. The support was prepared by solid-phase synthesis from functionalized beads by the introduction of a spacer chain followed by the att
- Barrett, Anthony G.M,De Miguel, Yolanda R
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- Amphiphilic conjugated thiophenes for self-assembling antenna systems in water
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Newly developed conjugated terthiophene surfactants are able to aggregate in water and to act as a host for hydrophobic chromophores, creating a multiple donor-acceptor energy transfer (ET) system by self-assembly.
- Van Rijn, Patrick,Savenije, Tom J.,Stuart, Marc C. A.,Van Esch, Jan H.
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Read Online
- Photochemical fabrication of three-dimensional micro- and nano-structured surfaces from a C60 monoadduct
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Exposure of Langmuir-Blodgett (LB) films of a C60 adduct supported on silicon wafers to UV light leads to cross-linking of the C 60 moieties, which are resistant to removal by solvent exposure, whereas unexposed moieties are readily removed. This process provides a convenient and simple route for the fabrication of highly conjugated surface-attached structures, with dimensions ranging from micrometres (using masks) to a few tens of nanometres using light emitted from a scanning near-field optical microscope (SNOM). The SNOM writing velocity was found to significantly affect the lateral resolution and the height of the three-dimensional nanostructures. Increasing the writing velocity from 0.3 to 2 μm s-1 resulted in a decrease in the width of the structures from 240 nm to 70 nm (corresponding to the SNOM aperture diameter), respectively, and a reduction in the height from 8 nm (the thickness of the original film) to 3 nm, respectively. This approach provides a simple, direct route to surface-bound nanometre scale assemblies of C60.
- Iqbal, Parvez,Sun, Shuqing,Hanwell, Marcus D.,Attwood, David,Leggett, Graham J.,Preece, Jon A.,Richardson, Tim H.,Tunnicliffe, David
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- Preparation of 7-methoxy tacrine dimer analogs and their in vitro/in silico evaluation as potential cholinesterase inhibitors
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Novel types of symmetric bis-7-methoxytacrines connected by oligoethyleneoxy chains 3-5 and nonsymmetric monomeric 7-methoxytacrines containing hydroxyl-terminated oligoethyleneoxy chains 6-8 were prepared, and their in vitro/in silico effects on human recombinant AChE (hAChE) and human plasmatic butyrylcholinesterase (hBChE) were compared, with 7-MEOTA (2) as the standard compound. The symmetric bis-7-MEOTA derivatives 3-5 showed hAChE inhibition similar to that of 2. On the other hand, their effects on hBChE revealed an increasing inhibition trend when the oligoethyleneoxy units between the two 7-MEOTA moieties became longer. Accordingly, compounds 4 and 5 showed better selectivity towards hBChE. The most effective in the inhibition hAChE and hBChE was compound 8 with the longest oligoethyleneglycol chain, whereas compounds 6 and 7 resulted in similar IC50 values. A molecular modeling study using substrates 5 and 8 showed a possible binding conformation and protein-ligand interaction between the substrates and AChE/BChE.
- Lee, Sang Kwang,Park, Min Kyun,Jhang, Ho Eun,Yi, Jinju,Nahm, Keepyong,Cho, Dae Won,Ra, Choon Sup,Musilek, Kamil,Horova, Anna,Korabecny, Jan,Dolezal, Rafael,Jun, Daniel,Kuca, Kamil Kuca
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- PYRROLO[2,3-B]PYRIDIN DERIVATIVES AS INHIBITORS OF INFLUENZA VIRUS REPLICATION
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Provided herein are compounds of Formula A, B or C that can inhibit the replication of influenza viruses, reduce the amount of influenza viruses, and/or treat influenza.
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Paragraph 00277
(2020/02/16)
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- PYRROLOPYRIMIDINE DERIVATIVES USEFUL AS INHIBITORS OF INFLUENZA VIRUS REPLICATION
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Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient a safe and effective amount of a compound represented by any of Formulas l-lll, or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a safe and effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.
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Paragraph 00296
(2018/11/22)
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- INHIBITORS OF HEPATITIS C VIRUS POLYMERASE
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The present invention provides, among other things, compounds represented by the general Formula I: (I) and pharmaceutically acceptable salts thereof, wherein L and A (and further substituents) are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.
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Paragraph 234; 235
(2016/10/11)
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- A practical and scalable process to selectively monofunctionalize water-soluble α,ω-diols
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A practical protocol for rapid and scalable synthesis of monofunctionalized α,ω-diols using a simple and inexpensive THP ether protection/deprotection strategy was described. Use of inexpensive DHP source and ease to remove excess water-soluble α,ω-diols
- Zhang, Quanxuan,Ren, Hong,Baker, Gregory L.
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supporting information
p. 3384 - 3386
(2014/06/09)
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- Synthesis of a library of propargylated and PEGylated α-hydroxy acids toward "clickable" polylactides via hydrolysis of cyanohydrin derivatives
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A new simple and practical protocol for scalable synthesis of a novel library of propargylated and PEGylated α-hydroxy acids toward the preparation of "clickable" polylactides was described. The overall synthesis starting from readily available propargyl alcohol, bromoacetaldehyde diethyl acetal, and OEGs or PEGs was developed as a convenient procedure with low cost and no need of column chromatographic purification. The terminal alkyne functionality survives from hydrolysis of the corresponding easily accessible cyanohydrin derivatives in methanolic sulfuric acid. Facile desymmetrization, monofunctionalization, and efficient chain-elongation coupling of OEGs further enable the incorporation of OEGs to α-hydroxy acids in a simple and efficient manner. At the end, synthesis of allyloxy lactic acid indicates that an alkene group is also compatible with the developed method. (Chemical Equation Presented).
- Zhang, Quanxuan,Ren, Hong,Baker, Gregory L.
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p. 9546 - 9555
(2015/02/19)
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- Zinc- and palladium-porphyrin based turnstiles
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The design and synthesis of two new Zn(ii) and Pd(ii) strapped-porphyrin based molecular turnstiles have been achieved. These molecules are based on a porphyrin backbone as a stator and a handle as a rotor. The junction between the two parts is ensured by covalent bonds using two opposite meso positions. Both compounds have been characterised in solution by NMR spectroscopy and in the solid state by X-ray diffraction on a single crystal. The dynamic of the two systems have been investigated in solution by 1- and 2-D NMR techniques such as ROESY. The switching between the open and closed states is described. Whereas for the Pd(ii) complex, the handle freely rotates around the stator, for the Zn(ii) analogue owing to the presence of a water molecule bound to the zinc atom and hydrogen bonded to the pyridyl moiety of the rotor, the rotation is blocked. The unlocking of the rotational movement was achieved using an external agent, mainly dimethylaminopyridine as a strong coordinating ligand.
- Lang, Thomas,Graf, Ernest,Kyritsakas, Nathalie,Hosseini, Mir Wais
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p. 112 - 118
(2013/02/22)
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- Synthesis of fulleropyrrolidine-imidazolium salt hybrids and their solubility in various organic solvents
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Eight types of fulleropyrrolidine-imidazolium hybrids have been synthesized and their solubility determined in various types of organic solvents. The solvent solubility of fullerene derivatives depends on the alky side chain on the imidazolium ring; modification of solvent solubility of the fulleropyrrolidine-imidazolium hybrids has thus been accomplished by introduction of an appropriate alkyl group using imidazoyl moiety as the 'functional group connector'. The imidazolium group seems to act not only as the connector but also as an important functional group that controls the solubility.
- Itoh, Toshiyuki,Mishiro, Makoto,Matsumoto, Kei,Hayase, Shuichi,Kawatsura, Motoi,Morimoto, Minoru
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p. 1823 - 1828
(2008/09/18)
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- Heat-sensitive compounds exhibitng a cloud point which can be used as extractants for the separation of metals in aqueous solution
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The invention relates to a heat-sensitive compound having the property of being soluble in water below a critical temperature Tc and insoluble in water above this temperature Tc, this property being thermally reversible, characterized in that it comprises a first amphiphilic and thermally reversible part corresponding to one of the following formulae (I) and (II): in which i is an integer ranging from 1 to 20 and j is an integer ranging from 3 to 30. This compound can be used to extract a chemical entity, such as uranium.
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Page/Page column 9-11
(2010/10/20)
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- Synthesis of oligo(ethylene glycol) toward 44-mer
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A synthetic method for oligo(ethylene glycol) toward 44-mer (FW = 1956.35) is described. Reiteration of Williamson's ether synthesis and hydrogenation to remove protecting benzyl group affords desired oligo(ethylene glycol) toward 44-mer in moderate yields. The advantages in this method are use of commercially easily available materials as starting materials and procedures avoiding difficulty in purification of the products as much as possible.
- Ahmed, Saleh A.,Tanaka, Mutsuo
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p. 9884 - 9886
(2007/10/03)
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- Lamellar liquid single crystal hydrogels: Synthesis and investigation of anisotropic water diffusion and swelling
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The synthesis and characterization of anisotropic liquid single crystal hydrogels (LSCHs) via photoinduced radical polymerization of magnetically aligned samples in the lyotropic mesophase are reported, which are stable against tensile stresses in all thr
- Kleinschmidt, Felix,Hickl, Markus,Saalwaechter, Kay,Schmidt, Claudia,Finkelmann, Heino
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p. 9772 - 9782
(2008/02/02)
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- Estrogen-linked platinum (II) complexes as anticancer agents
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wherein n may be 1, 2, 3, 4 or 5 when X is O, wherein n may be 2/3, 1, 4/3, 5/3, 2, 7/3, 8/3, 3, or 10/3 when X is C, wherein o may be 1, 2 or 3, wherein Y may be O or 17β-OH, wherein R1 may be selected from the group consisting of H, a straight alkyl group of 1 to 5 carbon atoms, a branched alkyl group of 3 to 5 carbon atoms, wherein R2 may be selected for the group consisting of H, a straight alkyl group of 1 to 4 carbon atoms, a branched alkyl group of 3 or 4 carbon atoms, F, Cl, Br, I, —CF3, —NO2, —OR1, —COR1 and —CH2OH. These compounds possess anticancer activity against hormono-dependent breast, uterus as well as ovarian cancer.
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Page/Page column 6
(2008/06/13)
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- Novel peripherally functionalized seco-porphyrazines: Synthesis, characterization and spectroscopic evaluation
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Co-macrocyclizations of 2,3-dipropylmaleonitrile and 2,3-di-(4- (methoxycarbonyl)phenyl)maleonitrile, respectively, with N,N′-dibenzyl-N, N′-di-(11-tetrahydropyranyloxy-3,6,9-trioxo-undecyl))maleonitrile and N,N,N′,N′-tetramethylmaleonitrile were used to prepare derivatives of the 4,5-diamino-porphyrazine systems including the zinc(II) complexes. Subsequent oxidation of the macrocycles with potassium permanganate gave the corresponding seco-porphyrazines. These were shown to be efficient sensitizers for the production of singlet oxygen (ΦΔ=0.15-0.57) by the determination of their photophysical properties.
- Sakellariou, Efstathia G.,Montalban, Antonio Garrido,Beall, Scott L.,Henderson, David,Meunier, Hubert G.,Phillips, David,Suhling, Klaus,Barrett, Anthony G. M.,Hoffman, Brian M.
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p. 9083 - 9090
(2007/10/03)
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- Polyaryl-poly(ethylene glycol) supports for solution-phase combinatorial synthesis
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The present invention is directed to the certain polyaryl-poly(ethylene glycol) compounds ("polyaryl-PEG" compounds) which are useful as soluble polyvalent supports in the preparation of combinatorial libraries of compounds. The resultant combinatorial li
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- Macrocyclic ethers by free radical cyclizations
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Tin hydride reduction of ω-iodo-polyoxaalkyl acrylates 1 using syringe pump addition of both reactants to a solution of AIBN in benzene at 80°C afforded the corresponding cyclic polyethers in excellent yields.
- Philippon, Annie,Tao, Jingchao,Tetard, David,Degueil-Castaing, Marie,Maillard, Bernard
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p. 2651 - 2682
(2007/10/03)
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