- Synthesis, characterization, and electrochemical study of a new tetradentate nickel(II)-Schiff base complex derived from ethylenediamine and 5′-(N-methyl-N-phenylaminomethyl)-2′-hydroxyacetophenone
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A tetradentate Schiff base ligand (3) has been synthesized via the reaction of 5′-(N-methyl-N-phenylaminomethyl)-2′-hydroxyacetophenone (2) with a stoichiometric amount of ethylenediamine in absolute ethanol. Compound 2 was prepared by reaction of 5′-chlo
- Ourari, Ali,Ouennoughi, Yasmina,Aggoun, Djouhra,Mubarak, Mohammad S.,Pasciak, Erick M.,Peters, Dennis G.
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Read Online
- Discovery of Novel Resorcinol Dibenzyl Ethers Targeting the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction as Potential Anticancer Agents
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Novel small molecule compounds based on various scaffolds including chalcone, flavonoid, and resorcinol dibenzyl ether were designed and tested for their inhibitory activity against the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 (PD-1/PD-L1) pathway. Among them, compound NP19 inhibited the human PD-1/PD-L1 interaction with IC50 values of 12.5 nM in homogeneous time-resolved fluorescence (HTRF) binding assays. In addition, NP19 dose-dependently elevated IFN-γproduction in a coculture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. Furthermore, NP19 displayed significant in vivo antitumor efficacy in two different mouse models of cancer (a melanoma B16-F10 tumor model and an H22 hepatoma tumor model). Moreover, H&E staining and flow cytometry data suggested that NP19 activated the immune microenvironment in the tumor, which may contribute to its antitumor effects. This work shows NP19 is a promising lead compound for further development as a new generation of small molecule inhibitors targeting the PD-1/PD-L1 pathway.
- Cheng, Binbin,Ren, Yichang,Niu, Xiaoge,Wang, Wei,Wang, Shuanghu,Tu, Yingfeng,Liu, Shuwen,Wang, Jin,Yang, Deying,Liao, Guochao,Chen, Jianjun
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Read Online
- A novel ferrocenic copper(II) complex Salen-like, derived from 5-chloromethyl-2-hydroxyacetophenone and N-ferrocenmethylaniline: Design, spectral approach and solvent effect towards electrochemical behavior of Fc+/Fc redox couple
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This paper reports the synthesis, spectroscopic characterizations and electrochemical behavior of the obtained tetradentate copper (II)-Schiff base complex with its two wings as ferrocenylaniline moieties. This new ferrocenic derivative with two ferroceny
- Ouennoughi, Yasmina,Karce, Houssam Eddine,Aggoun, Djouhra,Lanez, Touhami,Ruiz-Rosas, Ramiro,Bouzerafa, Brahim,Ourari, Ali,Morallon, Emilia
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Read Online
- Substituted biphenyl containing flavone and application thereof
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The invention relates to substituted biphenyl containing flavone, the chemical structure of the flavone is shown as in the following formula (I), R1 is methoxyl, N-acetyl ethanediamine, ethanediamine,piperazinyl, acetylpiperazine, ethyl piperazine, isopro
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Paragraph 0029; 0031-0033
(2019/02/26)
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- A substituted biphenyl chalcone and its application (by machine translation)
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The invention relates to a substituted biphenyl chalcone, the chalcone the chemical structure of the following formula (I) as shown by the, formula (I) in, R1 Is methoxy, N - acetyl di amino, piperazinyl, acetyl piperazinyl, ethyl piperazinyl, isopropyl piperazinyl, cyclopropyl piperazinyl, 1 - tert-butoxycarbonyl - 2 - methyl piperazinyl, cyclopropyl methyl piperazinyl or 1 - (3 - nitrophenyl) piperazinyl, R2 Hydrogen, fluoro or methyl, R3 Is hydrogen or a 1, 4 - dioxane-based. The invention claims a containing substituted biphenyl chalcone can be inhibiting programmed cell death receptor 1/programmed cell death ligand 1 (P D1/PD - L1) of the combined with each other, can be used for preparing PD1/PD - L1 inhibitors, the inhibitor of the effect. (by machine translation)
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Paragraph 0035; 0037-0040
(2019/03/28)
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- A fluorescent flavonoid for lysosome detection in live cells under "wash free" conditions
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Lysosomes are vital organelles in living cells, which have acidic environments (pH 4.0-5.0) where macrobiomolecules and malfunctioning organelles are broken down into monomers by hydrolase activity. The majority of the currently reported fluorescent probe
- Bertman, Keti Assor,Abeywickrama, Chathura S.,Baumann, Hannah J.,Alexander, Nicolas,McDonald, Lucas,Shriver, Leah P.,Konopka, Michael,Pang, Yi
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p. 5050 - 5058
(2018/08/17)
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- Synthesis and In Vitro Pharmacological Evaluation of 5-(Alkoxymethyl)-2-(3-alkylamino-2-hydroxypropoxy)phenylethanones Related to Acebutolol and Celiprolol
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The structure–activity relationships of 13 analogs of aryloxyaminopropanol type derived from 2-hydroxyphenylethanone as potential β-blockers are described. The synthesized compounds possess an isopropyl or a tert-butyl group in the hydrophilic part of the
- Bruchatá, Katarína,Némethy, Andrej,?i?máriková, Ru?ena,Ra?anská, Eva,Habala, Ladislav
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p. 733 - 740
(2016/10/12)
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- A step toward simplified detection of serum albumin on SDS-PAGE using an environment-sensitive flavone sensor
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In this study, we report a series of novel flavone-based sensors that exhibit a superior fluorescence response when interacting with serum albumin in real serum samples and in acrylamide gels. The detection limit of probe 4 for serum albumin solution is 0.09 μg mL-1, and the detectable volume for monkey serum reaches as low as 0.03 μL.
- Liu, Bin,Pang, Yi,Bouhenni, Rachida,Duah, Ernest,Paruchuri, Sailaja,McDonald, Lucas
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supporting information
p. 11060 - 11063
(2015/07/07)
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- New chalcones containing 5-fluorouracil exhibiting in vitro anti-cancer activity
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The synthesis and cytotoxicity evaluation of fourteen new chalcones containing 5-fluorouracil were introduced in which nine chalcones as Mannich bases 8a-i were synthesized from 2′-hydroxyacetophenone (1) in three steps including chloromethylation, N-alkylation and Claisen-Schmidt reactions. Other chalcones 14a-e were obtained from Click reaction between 1,3-dipropargyl-5-fluorouracil and azide derivatives of 2′,4′-dihydroxychalcone. The bio-assay results showed that 11 chalcones (excluding 8d, 8f and 8h) exhibited cytotoxicity against four human cancer cell lines including Hep-G2, RD, LU-1 and FL in which compound 14e exhibited the most potent cytotoxicity against Hep-G2, RD, LU-1 and FL with IC50 values of 1.48, 10.59, 3.64 and 7.02 μg/mL, respectively.
- Van Chinh, Luu,Hung, Truong Ngoc,Nga, Nguyen Thi,Phong, Le,Cuong, Le Huu,Chinh, Vu Tien,Kim, Soo Un,Vu, Tran Khac
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p. 251 - 261
(2015/06/23)
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- FLAVONOID COMPOUNDS OF LOW TOXICITY FOR BIOLOGICAL IMAGING APPLICATIONS
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Flavonoid compounds that are selective for a protein, a portion or a living cell, or a portion of an organism may be used as biological imaging agents. The flavonoid compounds are useful for methods of imaging organisms such as zebrafish embryos and zebra fish. Flavonoid compounds may also be used to detect protein. Advantageously, flavonoids that selectively bind protein, a portion of a living cell, or a portion of an organism may exhibit a florescence “turn-on” mechanism, where the flavonoids that are selectively bound exhibit a florescence response when excited.
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Paragraph 0111
(2016/03/09)
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- New chalcones containing nucleosides exhibiting in vitro anti-cancer activities
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Twenty-one new chalcones 9a-m (excluding 9e, 9j and 9l) and 10a-m (excluding 10j and 10l), containing nucleobases were synthesized from 2'-hydroxyacetophenone (1) by the reactions including chloromethylation, nucleophilic substitution with thymine and uracil, and Claisen-Schmidt reactions. These new chalcones were evaluated for in vitro cytotoxicity against five human cancer cell lines: SK-LU-1, Hep-G2, MCF7, SW480 and P388. The results showed that most of the tested chalcones exhibited inhibitory activity against five cancer cell lines except 10h, and 10i. Among the synthesized chalcones, compound 10c exhibited most potent cytotoxicity against MCF-7, SK-LU-1, SW480, HepG2 and P388 with IC50 values of 4.42, 4.81, 5.27, 3.67 and 4.11μg/mL, respectively.
- Van Chinh, Luu,Hung, Truong Ngoc,Nga, Nguyen Thi,Phong, Le,Huong, Le Mai,Ha, Tran Thi Hong,Kim, Soo Un,Vu, Tran Khac
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p. 534 - 545
(2014/05/20)
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- Synthesis and antimicrobial activity of chalcones containing benzotriazolylmethyl and imidazolylmethyl substituents
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Methods have been developed for the synthesis of new 1H-benzotriazol-1-ylmethyl- and 1H-imidazol-1-ylmethyl-substituted chalcones starting from 2-hydroxyacetophenone. The procedures include chloromethylation, N-alkylation, and Claisen-Schmidt condensation. The presence of an imidazole fragment on the ring A and piperazine fragment on the ring B of the resulting chalcones increases their antimicrobial activity (minimum inhibitory concentration 12.5-50.0 μg/mL), whereas introduction of a benzotriazole fragment reduces the antimicrobial activity.
- Chinh, L. V.,Hung, T. N.,Nga, N. T.,Mai, T. T. N.,Hang, T. T. N.,Tarasevich, V. A.
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p. 1767 - 1774
(2015/02/02)
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- Synthesis of unsymmetrical methylenebisphenol derivatives
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A simple and efficient route towards unsymmetrical methylenebisphenol derivatives is reported. This straightforward strategy avoids the use of harmful or dangerous chemicals, allowing the synthesis of highly functionalized bisphenyls with no need of protecting groups. The alkylation of the phenyl ring is selective for the para position of the hydroxyl substituent. All methylenebisphenols were obtained in a completely regioselective manner and isolated in high yields. Georg Thieme Verlag Stuttgart - New York.
- Guieu, Samuel,Rocha, Jo?o,Silva, Artur M. S.
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supporting information
p. 762 - 764
(2013/05/09)
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- PHARMACEUTICAL COMPOSITIONS FOR THE PREVENTION AND TREATMENT OF COMPLEX DISEASES AND THEIR DELIVERY BY INSERTABLE MEDICAL DEVICES
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The present invention relates to polyphenol-like compounds that are useful for inhibiting VCAM-1 expression, MCP-1 expression and/or SMC proliferation in a mammal. The disclosed compounds are useful for regulating markers of inflammatory conditions, including vascular inflammation, and for treatment and prevention of inflammatory and cardiovascular diseases and related disease states.
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Page/Page column 109-110
(2008/06/13)
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- (Hetero)aryl-bicyclic heteroaryl derivatives, their preparation and their use as protease inhibitors
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The present invention provides novel compounds of the Formula (I): A-B, its prodrug forms, or pharmaceutically acceptable salts thereof, wherein A represents a saturated, unsaturated, or a partially unsaturated bicyclic heterocyclic ring structure, and B represents an aryl or a heteroaryl group. Preferred compounds of the present invention comprise a benzimidazole or indole nucleus. The compounds of this invention are inhibitors of serine proteases, Urokinase (uPA), Factor Xa (FXa), and/or Factor VIIa (FVIIa), and have utility as anti cancer agents and/or as anticoagulants for the treatment or prevention of thromboembolic disorders in mammals.
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Page/Page column 64
(2010/02/11)
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- Synthesis, antiinflammatory and antibacterial activity of some new flavonoidal derivatives
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Several new flavones/flavanones and 5′-substituted-2′-hydroxy chalcones have been synthesised through Claisen Schmidt condensation. 5-Chloromethyl-2- hydroxy acetophenone 1 on condensation with various aromatic aldehydes yields chalcones 2a and 2b, which
- Khan,Hasan
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p. 1970 - 1974
(2007/10/03)
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