- Solvatochromic behavior of substituted 4-(nitrostyryl)phenolate dyes in pure solvents and in binary solvent mixtures composed of water and alcohols
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Several 4-(nitrostyryl)phenolates have been used recently as solvatochromic dyes in the investigation of pure solvents. Changes in their molecular structures allow a comparison of their solvation patterns to be made in different binary solvent mixtures, in an effort to relate structural factors to the preferential solvation (PS) observed in these media. Firstly, the solvatochromism of four of these probes was studied and a reversal in their solvatochromism was verified, which was expected following a comparison with other similar systems previously studied. The solvatochromic behavior of a series of twelve 4-(nitrostyryl)phenolate dyes was then investigated in water-alcohol mixtures. A sigmoid behavior was verified for one of the dyes in ethane-1,2-diol-water mixtures, and the dye was preferentially solvated by water in the alcohol-rich region. For all other mixture compositions a strong synergy was observed, with the PS of the dye molecules occurring through the less polar moiety of the water-alcohol aggregates in the binary mixtures. In addition, synergy was observed for some dyes, with PS occurring through the less polar moiety of the alcohol-water aggregates. For all of the other water-alcohol mixtures, the probes were preferentially solvated by the alcohol cosolvent. In order to quantify these deviations, a PS (or non-ideality) index PSI was proposed. The PSI values obtained correlated well with the hydrogen-bond donating ability of the alcoholic co-solvent, and also with the basicity of the phenolate dyes, and the trends observed were confirmed with data from the literature for two other phenolate dyes.
- Stock, Rafaela I.,Sandri, Crislaine,Rezende, Marcos C.,Machado, Vanderlei G.
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Read Online
- DNA mimics of red fluorescent proteins (RFP) based on G-quadruplex-confined synthetic RFP chromophores
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Red fluorescent proteins (RFPs) have emerged as valuable biological markers for biomolecule imaging in living systems. Developing artificial fluorogenic systems that mimic RFPs remains an unmet challenge. Here, we describe the design and synthesis of six
- Feng, Guangfu,Luo, Chao,Yi, Haibo,Yuan, Lin,Luo, Xingyu,Lei, Chunyang,Nie, Zhou,Yao, Shouzhuo,Lin, Bin,Hu, Xiaoxiao,Wang, Honghui
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- A Multicolor Large Stokes Shift Fluorogen-Activating RNA Aptamer with Cationic Chromophores
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Large Stokes shift (LSS) fluorescent proteins (FPs) exploit excited state proton transfer pathways to enable fluorescence emission from the phenolate intermediate of their internal 4-hydroxybenzylidene imidazolone (HBI) chromophore. An RNA aptamer named Chili mimics LSS FPs by inducing highly Stokes-shifted emission from several new green and red HBI analogues that are non-fluorescent when free in solution. The ligands are bound by the RNA in their protonated phenol form and feature a cationic aromatic side chain for increased RNA affinity and reduced magnesium dependence. In combination with oxidative functionalization at the C2 position of the imidazolone, this strategy yielded DMHBO+, which binds to the Chili aptamer with a low-nanomolar KD. Because of its highly red-shifted fluorescence emission at 592 nm, the Chili–DMHBO+ complex is an ideal fluorescence donor for F?rster resonance energy transfer (FRET) to the rhodamine dye Atto 590 and will therefore find applications in FRET-based analytical RNA systems.
- Steinmetzger, Christian,Palanisamy, Navaneethan,Gore, Kiran R.,H?bartner, Claudia
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- FLUORINE-CONTAINING COMPOUND AND ANTI-CANCER MEDICAL USE THEREOF
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The present invention provides a fluorine-containing compound shown in Formula II/III and its anti-cancer medical use.
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Paragraph 0071; 0074-0075
(2022/04/03)
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- Development of Near-Infrared Nucleic Acid Mimics of Fluorescent Proteins for in Vivo Imaging of Viral RNA with Turn-On Fluorescence
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GFP-like fluorescent proteins and their molecular mimics have revolutionized bioimaging research, but their emissions are largely limited in the visible to far-red region, hampering the in vivo applications in intact animals. Herein, we structurally modulate GFP-like chromophores using a donor-acceptor-acceptor (D-A-A′) molecular configuration to discover a set of novel fluorogenic derivatives with infrared-shifted spectra. These chromophores can be fluorescently elicited by their specific interaction with G-quadruplex (G4), a unique noncanonical nucleic acid secondary structure, via inhibition of the chromophores' twisted-intramolecular charge transfer. This feature allows us to create, for the first time, FP mimics with tunable emission in the near-infrared (NIR) region (Emmax = 664-705 nm), namely, infrared G-quadruplex mimics of FPs (igMFP). Compared with their FP counterparts, igMFPs exhibit remarkably higher quantum yields, larger Stokes shift, and better photostability. In a proof-of-concept application using pathogen-related G4s as the target, we exploited igMFPs to directly visualize native hepatitis C virus (HCV) RNA genome in living cells via their in situ formation by the chromophore-bound viral G4 structure in the HCV core gene. Furthermore, igMFPs are capable of high contrast HCV RNA imaging in living mice bearing a HCV RNA-presenting mini-organ, providing the first application of FP mimics in whole-animal imaging.
- Zhang, Jiaheng,Li, Huiyi,Lin, Bin,Luo, Xingyu,Yin, Peng,Yi, Ting,Xue, Binbin,Zhang, Xiao-Lian,Zhu, Haizhen,Nie, Zhou
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supporting information
p. 19317 - 19329
(2021/11/26)
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- 2-THIOXOTHIAZOLIDIN-4-ONE DERIVATIVES ACTIVE AS TRANSTHYRETIN LIGANDS AND USES THEREOF
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Compounds of formula (II) are provided for stabilizing protein transthyretin (TTR) and inhibiting amyloid fibril formation, for example, transthyretin-mediated amyloid fibril formation, and for treating, preventing, or ameliorating one or more symptoms of amyloid diseases, for example, transthyretin-related amyloidosis (ATTR).
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Paragraph 00307; 00308
(2016/06/15)
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- THIOARYL DERIVATIVES AS GPR120 AGONISTS
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The present invention relates to thioaryl derivatives of Formula 1 as defined in the specification, a method for preparing the same, a pharmaceutical composition comprising the same and use thereof. The thioaryl derivatives of Formula 1 according to the present invention promote GLP-1 formation in the gastrointestinal tract and improve insulin resistance in macrophages, pancreas cells, etc. due to anti-inflammatory action, and can accordingly be effectively used for preventing or treating diabetes, complications of diabetes, inflammation, obesity, non-alcoholic fatty liver, steatohepatitis or osteoporosis.
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Paragraph 331-332
(2014/05/24)
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- HYPOPHOSPHOROUS ACID DERIVATIVES HAVING ANTIHYPERALGIC ACTIVITY AND BIOLOGICAL APPLICATIONS THEREOF
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The invention relates to hypophosphorous acid derivatives of formula (I) wherein - X is H or OH, - R represents one or several radicals R1-R5, identical or different, two of R1-R5 optionally occupying the same position on the phenyl group, one to four of R1-R5 being H and the others being selected in the group comprising - 0-(CH2)n-COOH; - S-(CH2)n-COOH; -NH-(CH2)n-COOH; - 0-(CH,R') -COOH; -O- (CH2)n-OH; OR', -R' being a C1 -C3 alkyl radical;-OH; --COOH; halogen, particularly -F, - CI, -Br, -I, -CF3; -OCF3; -N02; -CH=CH-COOH; - -(CH2)n-COOH; O - (CH2)n- P03H2; O - (CF2)n- P03H2; O - (CH2)n- S03H; O - (CH2)n- CONHOH; O - (CH2)n-tetrazol; O - (CH2)n-hydroxyisoxazol - n = 1 to 5, preferably 1-3; said hypophosrous acid derivatives being diastereoisomers or enantiomers.
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Page/Page column 26
(2012/12/13)
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- Peroxynitrite generation from a NO-releasing nitrobenzene derivative in response to photoirradiation
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Photocontrollable ONOO- generation from a nitrobenzene derivative was demonstrated. The designed compound released NO in response to photoirradiation, and the resulting semiquinone reduced molecular oxygen to generate O2-; reaction of the two generated ONOO -, as confirmed with an ONOO- fluorescent probe, HKGreen-3.
- Ieda, Naoya,Nakagawa, Hidehiko,Horinouchi, Taeko,Peng, Tao,Yang, Dan,Tsumoto, Hiroki,Suzuki, Takayoshi,Fukuhara, Kiyoshi,Miyata, Naoki
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supporting information; experimental part
p. 6449 - 6451
(2011/06/27)
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- GPR120 RECEPTOR AGONISTS AND USES THEREOF
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GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.
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Page/Page column 82-83
(2012/01/06)
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- GPR120 RECEPTOR AGONISTS AND USES THEREOF
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GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.
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Page/Page column 24-25
(2012/01/13)
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- Light Emitting Polymer Devices Using Self-Assembled Monolayer Structures
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A light emitting device comprising a transparent substrate; a layer of conducting material in contact with the transparent substrate; a self-assembled monolayer bonded to the layer of conducting material; one or more light emitting polymer layers in electron contact to the self-assembled monolayer; and a reflective metal layer in electron contact with the light emitting polymer layer is provided. The light emitting device provided gives enhanced performance as compared to currently available devices. Also provided is a self-assembled monolayer having the formula: R2-R3—Y where Y is a group capable of electron contact with a light emitting polymer, R3 contains a conjugated group, and R2 is a group capable of bonding to a conducting material.
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- ARYL GPR120 RECEPTOR AGONISTS AND USES THEREOF
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Aryl GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.
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Page/Page column 75-76
(2010/05/13)
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- GPR120 RECEPTOR AGONISTS AND USES THEREOF
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GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.
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Page/Page column 58
(2010/08/04)
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- 1,3-Diphenylprop-2-En-1-One Derivative Compounds, Preparation Method Thereof and Uses of Same
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The invention relates to substituted 1,3-diphenylprop-2-en-1-one derivative compounds, pharmaceutical and/or cosmetic compositions containing same, and the applications thereof in therapeutics and cosmetics. The invention also relates to a method for prep
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Page/Page column 23
(2008/06/13)
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- Synthesis and anticancer activity of fluorinated analogues of combretastatin A-4
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The synthesis of a series of fluorinate d benzaldehydes and their use in the Wittig synthesis of fluoro-substituted stilbenes is described. 3,5-Difluoro-4-hydroxybenzaldehyde (6) and 3-fluoro-4-methoxybenzaldehyde (11) are prepared by Duff formylation of 3,5-difluorophenol and 2-fluoroanisole, respectively. 2-Methoxy-3,4-difluorobenzaldehyde was obtained by Friedel-Crafts formylation of 2,3-difluoroanisole with α,α-dichloromethyl methyl ether. The aldehydes were used to make a series of fluorinated analogues of the anticancer combretastatins A-1, A-2 and A-4. The in vitro anticancer properties of the fluoro combretastatins are reported. The most active fluoro analogue 3-deoxy-3-fluoro-combretastatin A-4 (Z-2) retains the potent cell growth inhibitory properties of CA-4.
- Lawrence, Nicholas J.,Hepworth, Lucy A.,Rennison, David,McGown, Alan T.,Hadfield, John A.
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p. 101 - 108
(2007/10/03)
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- A convenient route to new fluorinated photodynamic therapeutic photosensitizers based on meso-tetra(hydroxyphenyl)porphyrins
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A general synthetic route was developed for the synthesis of new fluorinated tetra(hydroxyphenyl) porphyrins [5,10,15,20-tetrakis(2-fluoro-3-hydroxyphenyl)porphyrin 10, 5,10,15,20-tetrakis(2,4-difluoro-3-hydroxyphenyl)porphyrin 11, and 5,10,15,20-tetrakis(3,5-difluoro-4-hydroxyphenyl)porphyrin 12], analogues of sensitisers 1-3 which are known to be active in vivo in cancer photodynamic therapy.
- Songca, Sandile P.,Bonnett, Raymond,Maes, Catherine M.
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- Synthesis and Structure-Activity Studies of Some Disubstituted Phenylisoxazoles against Human Picornavirus
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A number 2,6-disubstituted analogues of disoxaril, a broad spectrum antipicornavirus agent, have been prepared and evaluated against several rhinovirus serotypes.A QSAR study revealed that the mean MIC () against five rhinovirus serotypes correlated well with log P.The 2,6-dichloro analogue, 15, was highly effective in vitro against rhinoviruses with an MIC80 of 0.3 μM, as well as against several enteroviruses, and was also effective in preventing paralysis in mice infected with coxsackievirus A-9.
- Diana, Guy D.,Cutcliffe, David,Oglesby, Richard C.,Otto, Michael J.,Mallamo, John P.,et al.
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p. 450 - 455
(2007/10/02)
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