60221-37-6Relevant academic research and scientific papers
Preparation, Single-Molecule Manipulation, and Energy Transfer Investigation of a Polyfluorene-graft-DNA polymer
Madsen, Mikael,Christensen, Rasmus S.,Krissanaprasit, Abhichart,Bakke, Mette R.,Riber, Camilla F.,Nielsen, Karina S.,Zelikin, Alexander N.,Gothelf, Kurt V.
, p. 10511 - 10515 (2017)
Conjugated polymers have been intensively studied due to their unique optical and electronic properties combined with their physical flexibility and scalable bottom up synthesis. Although the bulk qualities of conjugated polymers have been extensively utilized in research and industry, the ability to handle and manipulate conjugated polymers at the nanoscale lacks significantly behind. Here, the toolbox for controlled manipulation of conjugated polymers was expanded through the synthesis of a polyfluorene-DNA graft-type polymer (poly(F-DNA)). The polymer possesses the characteristics associated with the conjugated polyfluorene backbone, but the protruding single-stranded DNA provides the material with an exceptional addressability. This study demonstrates controlled single-molecule patterning of poly(F-DNA), as well as energy transfer between two different polymer–DNA conjugates. Finally, highly efficient DNA-directed quenching of polyfluorene fluorescence was shown.
Internalization of a peptide into multilamellar vesicles assisted by the formation of an α-Oxo oxime bond
Richard, Antoine,Bourel-Bonnet, Line
, p. 7315 - 7321 (2005)
As part of a drug-delivery project, we designed and synthesised a novel hydroxylamine cholesterol-based anchor to ensure the chemoselective ligation of recognition patterns onto multilamellar vesicles by oxime ligation. The entry of a glyoxylyl peptide in
A synthetic 2,3-diarylindole induces microtubule destabilization and G2/M cell cycle arrest in lung cancer cells
Thanaussavadate, Bongkotrat,Ngiwsara, Lukana,Lirdprapamongkol, Kriengsak,Svasti, Jisnuson,Chuawong, Pitak
supporting information, (2019/11/14)
The anticancer potential of a synthetic 2,3-diarylindole (PCNT13) has been demonstrated in A549 lung cancer cells by inducing both apoptosis and autophagic cell death. In this report, we designed to connect a fluorophore to the compound via a hydrophilic linker for monitoring intracellular localization. The best position for linker attachment was identified from cytotoxicity and effect on cell morphology of newly synthesized PCNT13 derivatives bearing hydrophilic linker. Cytotoxicity and effect on cell morphology related to the parental compound were used to identify the optimum position for linker attachment in the PCNT13 chemical structure. The fluorophore-PCNT13 conjugate was found to localize in the cytoplasm. Microtubules were found to be one of the cytosolic target proteins of PCNT13, as the compound could inhibit tubulin polymerization in vitro. A molecular docking study revealed that PCNT13 binds at the colchicine binding site on the α/β-tubulin heterodimer. The effect of PCNT13 on microtubule dynamics caused cell cycle arrest in the G2/M phase as analyzed by flow cytometric analysis.
PYRROLO[2,3-B]PYRIDIN DERIVATIVES AS INHIBITORS OF INFLUENZA VIRUS REPLICATION
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Paragraph 00261, (2020/02/16)
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.
PYRROLOPYRIMIDINE DERIVATIVES USEFUL AS INHIBITORS OF INFLUENZA VIRUS REPLICATION
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Paragraph 00280, (2018/11/22)
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.
INHIBITORS OF HEPATITIS C VIRUS POLYMERASE
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Paragraph 234; 235, (2016/10/11)
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.
Synthesis of TEG-Substituted 4-(N-Methyl-N-Boc-amino)styrylpyridine as Key Precursor for Monodentate and Multidentate Imaging Agents for A β Plaques
Li, Zhi,Liu, Bo,Duan, Wubiao,Zhu, Lin
supporting information, p. 2740 - 2747 (2015/12/18)
Triethylene glycol (TEG)-substituted 4-(N-methyl-N-Boc-amino)styrylpyridine, which can serve as key precursor for many monodentate and multidentate imaging agents for Aβ plaques in the human brain, has been readily synthesized with cheap starting materials. Our new method could be employed for mass production of monodentate imaging agent AV-45 and other multidentate imaging agents.
Preparation of 7-methoxy tacrine dimer analogs and their in vitro/in silico evaluation as potential cholinesterase inhibitors
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
, p. 1654 - 1660 (2015/07/15)
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.
Designer nanorings with functional cavities from self-assembling β-Sheet peptides
Park, Il-Soo,Yoon, You-Rim,Jung, Minseon,Kim, Kimoon,Park, Seongbyeong,Shin, Seokmin,Lim, Yong-Beom,Lee, Myongsoo
supporting information; experimental part, p. 452 - 458 (2011/10/03)
β-Barrel proteins that take the shape of a ring are common in many types of water-soluble enzymes and water-insoluble transmembrane pore-forming proteins. Since β-barrel proteins perform diverse functions in the cell, it would be a great step towards developing artificial proteins if we can control the polarity of artificial β-barrel proteins at will. Here, we describe a rational approach to construct β-barrel protein mimics from the self-assembly of peptide-based building blocks. With this approach, the direction of the self-assembly process toward the formation of water-soluble β-barrel nanorings or water-insoluble transmembrane β-barrel pores could be controlled by the simple but versatile molecular manipulation of supramolecular building blocks. This study not only delineates the basic driving force that underlies the folding of β-barrel proteins, but also lays the foundation for the facile fabrication of β-barrel protein mimics, which can be developed as nanoreactors, ion- and small-molecule-selective pores, and novel antibiotics. Copyright
Design and synthesis of Sn-porphyrin based molecular gates
Guenet, Aurelie,Ernest Graf,Nathalie Kyritsakas,Hosseini, Mir Wais
scheme or table, p. 1872 - 1883 (2010/05/01)
The design, synthesis, and structural characterization, both in solution by 1H NMR and in the solid state by X-ray diffraction on single crystals, of a series of molecular gates based on Sn-porphyrin derivatives are presented. The molecular systemis based on a porphyrin core bearing at the meso positions either phenyl or pyridyl groups as a stator, octahedral Sn(IV) cation located at the center of the porphyrin as a hinge, and different handles connected to the porphyrin through Sn-O axial bonds. The stability of the complexes in the presence of different acids is also reported.
