30787-43-0Relevant academic research and scientific papers
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
Ourari, Ali,Ouennoughi, Yasmina,Aggoun, Djouhra,Mubarak, Mohammad S.,Pasciak, Erick M.,Peters, Dennis G.
, p. 59 - 64 (2014)
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
Discovery of Novel Resorcinol Dibenzyl Ethers Targeting the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction as Potential Anticancer Agents
Cheng, Binbin,Ren, Yichang,Niu, Xiaoge,Wang, Wei,Wang, Shuanghu,Tu, Yingfeng,Liu, Shuwen,Wang, Jin,Yang, Deying,Liao, Guochao,Chen, Jianjun
, p. 8338 - 8358 (2020)
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.
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
Ouennoughi, Yasmina,Karce, Houssam Eddine,Aggoun, Djouhra,Lanez, Touhami,Ruiz-Rosas, Ramiro,Bouzerafa, Brahim,Ourari, Ali,Morallon, Emilia
, p. 344 - 351 (2017)
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
Substituted biphenyl containing flavone and application thereof
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Paragraph 0029; 0031-0033, (2019/02/26)
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
A substituted biphenyl chalcone and its application (by machine translation)
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Paragraph 0035; 0037-0040, (2019/03/28)
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)
A fluorescent flavonoid for lysosome detection in live cells under "wash free" conditions
Bertman, Keti Assor,Abeywickrama, Chathura S.,Baumann, Hannah J.,Alexander, Nicolas,McDonald, Lucas,Shriver, Leah P.,Konopka, Michael,Pang, Yi
, p. 5050 - 5058 (2018/08/17)
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
Synthesis and In Vitro Pharmacological Evaluation of 5-(Alkoxymethyl)-2-(3-alkylamino-2-hydroxypropoxy)phenylethanones Related to Acebutolol and Celiprolol
Bruchatá, Katarína,Némethy, Andrej,?i?máriková, Ru?ena,Ra?anská, Eva,Habala, Ladislav
, p. 733 - 740 (2016/10/12)
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
A step toward simplified detection of serum albumin on SDS-PAGE using an environment-sensitive flavone sensor
Liu, Bin,Pang, Yi,Bouhenni, Rachida,Duah, Ernest,Paruchuri, Sailaja,McDonald, Lucas
supporting information, p. 11060 - 11063 (2015/07/07)
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.
New chalcones containing 5-fluorouracil exhibiting in vitro anti-cancer activity
Van Chinh, Luu,Hung, Truong Ngoc,Nga, Nguyen Thi,Phong, Le,Cuong, Le Huu,Chinh, Vu Tien,Kim, Soo Un,Vu, Tran Khac
, p. 251 - 261 (2015/06/23)
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.
FLAVONOID COMPOUNDS OF LOW TOXICITY FOR BIOLOGICAL IMAGING APPLICATIONS
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Paragraph 0111, (2016/03/09)
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.
