- Reinvestigation of the synthesis of “covalent-assembly” type probes for fluoride ion detection. Identification of novel 7-(diethylamino)coumarins with aggregation-induced emission properties
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An unprecedented C-3 functionalization of 4-(diethylamino)salicylaldehyde through a Friedel-Crafts type alkylation reaction has been discovered during the synthesis of “covalent-assembly”-based fluorescent probes for detection of fluoride ions. The resulting Friedel-Crafts adduct was successfully used for the preparation of two novel 8-substituted 7-(diethylamino)coumarin dyes. The photophysical study of these fluorophores has enabled us to highlight their remarkable aggregation-induced emission (AIE) properties characterized by a yellow-orange emission of aggregates in water. Therefore, 4-(tert-butyldimethylsilyloxy)benzyl substituent was identified as a novel AIE-active moiety which could be seen as a possible alternative to popular tetraphenylethylene (TPE).
- Quesneau, Valentin,Roubinet, Beno?t,Renard, Pierre-Yves,Romieu, Anthony
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Read Online
- Discovery of Novel N-(4-Hydroxybenzyl)valine Hemoglobin Adducts in Human Blood
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Humans are exposed to a wide range of electrophilic compounds present in our diet and environment or formed endogenously as part of normal physiological processes. These electrophiles can modify nucleophilic sites of proteins and DNA to form covalent addu
- Degner, Amanda,Carlsson, Henrik,Karlsson, Isabella,Eriksson, Johan,Pujari, Suresh S.,Tretyakova, Natalia Y.,T?rnqvist, Margareta
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- Novel methinic functionalized and dendritic C-scorpionates
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The study of chelating ligands is undoubtedly one of the most significant fields of research in chemistry. The present work is directed to the synthesis of new functionalized derivatives of tripodal C-scorpionate compounds. Tris-2,2,2-(1-pyrazolyl)ethanol, HOCH2C(pz)3 (1), one of the most important derivatives of hydrotris(pyrazolyl)methane, was used as a building block for the synthesis of new functionalized C-scorpionates, aiming to expand the scope of this unexplored class of compounds. The first dendritic C-scorpionate was successfully prepared and used in the important industrial catalytic reactions, Sonogashira and Heck C-C cross-couplings.
- Martins, Luísa M.D.R.S.,Wanke, Riccardo,Silva, Telma F.S.,Pombeiro, Armando J.L.,Servin, Paul,Laurent, Régis,Caminade, Anne-Marie
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Read Online
- KRAS G12D INHIBITORS
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The present invention relates to compounds that inhibit KRas G12D. In particular, the present invention relates to compounds that inhibit the activity of KRas G12D, pharmaceutical compositions comprising the compounds and methods of use therefor.
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Paragraph 0964
(2021/03/05)
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- Synthesis of N-benzyl substituted 1,4-imino-L-lyxitols with a basic functional group as selective inhibitors of Golgi α-mannosidase IIb
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Inhibition of the biosynthesis of complex N-glycans in the Golgi apparatus is one of alternative ways to suppress growth of tumor tissue. Eight N-benzyl substituted 1,4-imino-L-lyxitols with basic functional groups (amine, amidine, guanidine), hydroxyl an
- Klunda, Tomá?,?esták, Sergej,Kóňa, Juraj,Poláková, Monika
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p. 424 - 431
(2018/11/23)
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- Fluorescent probe for detecting fluoride ions
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The invention discloses a fluorescent probe for detecting fluoride ions in an organism, and belongs to the technical field of analytical chemistry. The fluorescent probe uses a cyanine dye QCy7 as a parent body, a silicon-oxygen bond as a switch and hydroxybenzyl as a linker, and the chemical structure general formula of the fluorescent probe is as shown in a formula (I). The fluorescent probe hassimple synthesis and is convenient to use, can specifically react with the fluoride ions, breaks the silicon-oxygen bond, and releases fluorescence of fluorogen QCy7 through electron transfer. The fluorescent probe is not interfered with other ions in the process of detecting the fluoride ions, has good selectivity to the fluoride ions, and can accurately detect the fluoride ions in the organism.
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- Method for identifying fluorine-containing toothpaste by naked eyes through probe S-F
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The invention relates to a method for identifying fluorine-containing toothpaste by naked eyes through a probe S-F. The structure of the probe is as follows: the formula is shown in the description. After the probe is added into a toothpaste sample, wheth
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- Indazole-oxadiazole derivative, medicinal composition containing derivative, and application of derivative in tumor prevention
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The invention discloses an indazole-oxadiazole derivative with the structure represented by general formula a shown in the description, or a pharmaceutically acceptable salt or solvate thereof. In the formula, X is O or N, Y is N, Z is N or O, and all groups are as defined in the description. The invention also discloses a medicinal composition adopting the derivative as an active component, and a use of the derivative. Compounds synthesized in the invention have an HIF-1 inhibition effect, and most of the compounds have a substantial HIF-1 inhibition effect, have strong in-vivo and in-vitro anti-HIF-1 effect on human colorectal carcinoma cell strains (HCT116) and other tumor cell strains, and can be used for treating tumor diseases.
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Paragraph 0249; 0250; 0251; 0252
(2017/07/25)
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- Total Synthesis of Two Glycosylated Stilbenes, Oxyresveratrol 2-O-β- d -Glucopyranoside and 2,3,5,4′-Tetrahydroxystilbene 2-O-β- d -Glucopyranoside
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Glycosylated stilbenes are biologically active secondary metabolites of plants and have the potential to alleviate a broad range of human diseases. However, some of these compounds are not naturally abundant, and thus the synthesis of such molecules is de
- Kumar, Sunil,Lee, Hsueh-Yun,Liou, Jing-Ping
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p. 1294 - 1301
(2017/05/31)
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- Resveratrol derivative containing fluorine group, and preparation method and application
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The invention belongs to the technical field of medicines and discloses a resveratrol derivative containing a fluorine group, and a preparation method and an application. The resveratrol derivative has the structural characteristics as shown in a general
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- AZASULFURYLPEPTIDE-BASED CD36 MODULATORS AND USES THEREOF
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Novel azasulfuryl-containing peptidomimetics capable of inhibiting CD36 activity are disclosed. Use of these azasulfuryl-containing peptidomimetics for the treatment of CD36-related diseases, disorders or conditions, including TLR2-mediated inflammatory disease, disorder or condition, and methods of obtaining such azasulfuryl-containing peptidomimetics, are also disclosed.
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- 4 - hydroxy-benzyl vitamin A one method for the synthesis of (by machine translation)
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The invention relates to synthesis for three compounds namely 4-hydroxybenzyl vitamin A ketone (4-HBR), 4-(tert-butyldimethyl silica) benzyl bromide and vitamin A hydroxynitrile protected by tert-butyldimethyl silicon, and synthesis for a compound obtaine
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Paragraph 0015; 0017; 0018; 0019; 0020
(2016/11/14)
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- Synthesis, electrochemistry and anticancer activity of novel ferrocenyl phenols prepared via azide-alkyne 1,3-cycloaddition reaction
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A series of monophenols and diphenols containing the ferrocene-C triazolyl and ferrocene-Ntriazolyl bond were prepared in a cycloaddition reaction of ethynylferrocene with aryl and benzyl azides and in a reaction of azidoferrocene with phenylacetylenes, respectively. The anticancer activity of the prepared compounds against hormone-dependent (MCF-7) and hormone-independent (HCC38) breast cancer cell lines was studied. The investigated compounds exhibited moderate anticancer activity against hormone-independent (IC50 ~ 15-48 μM) cancer cell line and low activity against hormone-dependent cancer cell line (IC50 ~ 84-98 μM).
- Plazuk, Damian,Rychlik, B?azej,B?auz, Andrzej,Domaga?a, S?awomir
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p. 102 - 112
(2012/09/07)
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- Use of Dendrimers to Stimulate Cell Growth
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The present invention relates to the use of dendrimers with monophosphonic or bisphosphonic terminations in order to stimulate the growth of cell cultures or to activate cells in culture.
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Page/Page column 86-87
(2009/06/27)
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- Integrase inhibitors
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Tricyclic compounds, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed.
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Page/Page column 36-37
(2008/06/13)
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- 5-Pyrrolidinylsulfonyl isatins as a potential tool for the molecular imaging of caspases in apoptosis
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Caspases are the unique enzymes responsible for the execution of the cell death program and may represent an exclusive target for the specific molecular imaging of apoptosis in vivo. 5-Pyrrolidinylsulfonyl isatins represent potent nonpeptidyl caspase inhibitors that may be suitable for the development of caspase binding radioligands (CBRs). (S)-5-[1-(2-Methoxymethylpyrrolidinyl) sulfonyl]isatin (7) served as a lead compound for modification of its N-1-position. Corresponding pairs of N-1-substituted 2-methoxymethyl- and 2-phenoxymethylpyrrolidinyl derivatives were examined in vitro by biochemical caspase inhibition assays. All target compounds possess high in vitro caspase inhibition potencies in the nanomolar to subnanomolar range for caspase-3 (Ki = 0.2-56.1 nM). As shown for compound (S)-1-(4-(2-fluoroethoxy) benzyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin (35), the class of N-1-substituted 5-pyrrolidinylsulfonyl isatins competitively inhibits caspase-3. All caspase inhibitors show selectivity for the effector caspases-3 and -7 in vitro. The 2-methoxymethylpyrrolidinyl versions of the isatins appear to possess superior caspase inhibition potencies in cellular apoptosis inhibition assays compared with the 2-phenoxymethylpyrrolidinyl inhibitors.
- Kopka, Klaus,Faust, Andreas,Keul, Petra,Wagner, Stefan,Breyholz, Hans-J?rg,H?ltke, Carsten,Schober, Otmar,Sch?fers, Michael,Levkau, Bodo
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p. 6704 - 6715
(2007/10/03)
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- An unhydrolyzable analogue of N-(4-hydroxyphenyl)retinamide: Synthesis and preliminary biological studies
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The synthesis of a nonhydrolyzable, carbon-linked analogue (4-HBR) of the retinoid N-(4-hydroxyphenyl)retinamide (4-HPR) using Umpolung methods is described. Preliminary studies of biological activity show 4-HBR is similar to 4-HPR in its actions although a potentially relevant and desirable difference is its reduced suppression of plasma vitamin A levels. These results show that 4-HPR does not have to be hydrolyzed to retinoic acid to produce its chemotherapeutic effects. Elsevier Science Ltd. All rights reserved.
- Weiss, Kevin L.,Alshafie, Galal,Chapman, Jason S.,Mershon, Serena M.,Abou-Issa, Hussein,Clagett-Dame, Margaret,Curley Jr., Robert W.
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p. 1583 - 1586
(2007/10/03)
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- C-linked analogs of N-(4-hydroxyphenyl) retinamide
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Disclosed are acid-stable compounds of Formula I: as well as pharmaceutical compositions containing the compounds as active ingredients, and methods to treat cancers in mammal, including humans, by administering one or more of the compounds to a subject i
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- Chemi- and bioluminescence of coelenterazine analogues possessing an adamantylmethyl group
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Coelenterazine analogues possessing the adamantylmethyl group at the C2 or C8 position were prepared to study their effects on chemi- and bioluminescence. Stability of the excited state coelenteramide analogues was significantly affected by the substituti
- Hirano, Takashi,Negishi, Ryo,Yamaguchi, Mihoko,Chen, Feng Qi,Ohmiya, Yoshihiro,Tsuji, Frederick I.,Ohashi, Mamoru
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p. 12903 - 12916
(2007/10/03)
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- Potential photoaffinity labels for tubulin. Synthesis and evaluation of diazocyclohexadienone and azide analogs of colchicine, combretastatin, and 3,4,5-trimethoxybiphenyl
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Analogs of tubulin assembly inhibitors such as colchicine, combretastatin, and 3,4,5-trimethoxybiphenyl which incorporate a 6-diazo-2,4-cyclohexadienone (o-quinone diazide) ring have been synthesized and characterized. The compounds synthesized include 6-diazo-4-(2',3',4'-trimethoxyphenyl)cyclohexa-2,4-dien-1-one and its 3-methyl and 3-ethyl analogs (1a-c), 6-diazo-3-(2,3,4-trimethoxyphenyl)-2,4-cyclohexadien-1-one and its 4-methyl and 4-ethyl derivatives (2a-c), 4-[Z-2-(3',4',5'-trimethoxyphenyl)ethenyl]-6-diazocyclohexa-2,4-dienon e (3), 3-[Z-2-(3',4',5'-trimethoxyphenyl)ethenyl]-6-diazocyclohexa-2,4-dien-1 -one (4), the corresponding dihydro derivatives (5, 6) and two isomeric diazocyclohexadienones derived from N-acetylcolchinol (7, 8). Compounds in which the cyclohexadienone oxygen is approximately isostructural with carbonyl or hydroxy functions of the parent compounds exhibit good activity in the tubulin assembly inhibition assay. 2'-Alkyl-4'azido-3,4,5-trimethoxy-1,1'-biphenyls also show good activity as tubulin assembly inhibitors.
- Olszewski,Marshalla,Sabat,Sundberg
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p. 4285 - 4296
(2007/10/02)
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- 2-Pyrrolidinone derivatives as HIV protease inhibitors
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Compounds of the form,ψ ψ A-B-G-Jψ ψ wherein A is an amine protecting group and the like, B an amino acid or analog thereof, wherein G is ψψ ψand J a small terminal group are described. These compounds are useful in the inhibition of HIV protease, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.ψ
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