149683-53-4Relevant academic research and scientific papers
Metal- And additive-free C-H oxygenation of alkylarenes by visible-light photoredox catalysis
García Manche?o, Olga,Kuhlmann, Jan H.,Pérez-Aguilar, María Carmen,Piekarski, Dariusz G.,Uygur, Mustafa
supporting information, p. 3392 - 3399 (2021/05/21)
A metal- and additive-free methodology for the highly selective, photocatalyzed C-H oxygenation of alkylarenes under air to the corresponding carbonyls is presented. The process is catalyzed by an imide-acridinium that forms an extremely strong photooxidant upon visible light irradiation, which is able to activate inert alkylarenes such as toluene. Hence, this is an easy to perform, sustainable and environmentally friendly oxidation that provides valuable carbonyls from abundant, readily available compounds.
Rhodium-Catalyzed Deoxygenation and Borylation of Ketones: A Combined Experimental and Theoretical Investigation
Tao, Lei,Guo, Xueying,Li, Jie,Li, Ruoling,Lin, Zhenyang,Zhao, Wanxiang
supporting information, p. 18118 - 18127 (2020/11/26)
The rhodium-catalyzed deoxygenation and borylation of ketones with B2pin2 have been developed, leading to efficient formation of alkenes, vinylboronates, and vinyldiboronates. These reactions feature mild reaction conditions, a broad substrate scope, and excellent functional-group compatibility. Mechanistic studies support that the ketones initially undergo a Rh-catalyzed deoxygenation to give alkenes via boron enolate intermediates, and the subsequent Rh-catalyzed dehydrogenative borylation of alkenes leads to the formation of vinylboronates and diboration products, which is also supported by density functional theory calculations.
BRM TARGETING COMPOUNDS AND ASSOCIATED METHODS OF USE
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Paragraph 1073-1074, (2019/10/23)
The present disclosure relates to bifunctional compounds, which find utility as modulators of SMARCA2 or BRM (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand that binds to the Von Hippel-Lindau E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
Multienzyme One-Pot Cascade for the Stereoselective Hydroxyethyl Functionalization of Substituted Phenols
Payer, Stefan E.,Pollak, Hannah,Schmidbauer, Benjamin,Hamm, Florian,Juri?i?, Filip,Faber, Kurt,Glueck, Silvia M.
supporting information, p. 5139 - 5143 (2018/09/13)
The operability and substrate scope of a redesigned vinylphenol hydratase as a single biocatalyst or as part of multienzyme cascades using either substituted coumaric acids or phenols as stable, cheap, and readily available substrates are reported.
Synthetic method for rugchalcone A, B and their derivatives and their anti-inflammatory use
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Paragraph 0059-0060, (2017/08/09)
The present invention provides an effective anti-inflammatory agent which does not have a side effect. The present inventors have invented an effective method for synthesizing 2-aroylbenzofuran, rugchalcone A, B, and a derivative thereof at high yield by a Rap-Stoermer reaction between substituted salicylaldehyde and phenacyl bromide. Moreover, the inventors have evaluated an anti-inflammatory effect of the compound in lipopolysaccharide-induced RAW 264.7 macrophages. The compound remarkably inhibits the generation of nitrogen oxide which mediates inflammation without having cytotoxicity at a concentration of 10 andmu;M, and an IC_50 value is in the range of 0.57-13.27 andmu;M. From 2-aroylbenzofuran synthesized according to the preset invention, compound 4 (99.6%; IC_50 = 0.57), rugchalcone B (compound 2)(99.3%; IC_50 = 4.13), compound 7 (96.8%; IC_50 = 1.90), and compound 8 (74.3%; IC_50 = 0.99) show a maximum inhibiting activity. Such a result shows that compounds 2, 4, 7, and 8 having 4-hydroxyphenyl group and/or a hydroxyl group in a 5- and/or 6- position of a benzofuran motif can be functioned as a structure needed in developing an iNOS inhibitor with respect to the application thereof to the anti-inflammatory field.COPYRIGHT KIPO 2017
Platinum(ii) O,S complexes as potential metallodrugs against Cisplatin resistance
Hildebrandt, Jana,H?fner, Norman,G?rls, Helmar,Kritsch, Daniel,Ferraro, Giarita,Dürst, Matthias,Runnebaum, Ingo B.,Merlino, Antonello,Weigand, Wolfgang
supporting information, p. 18876 - 18891 (2016/12/09)
We report on platinum(ii) complexes with different cinnamic acid derivatives as ligands with cytotoxic activity against Cisplatin resistant ovarian cancer cell line subcultures of SKOV3 and A2780. A typical mechanism of action for platinum(ii) complexes a
Synthesis and biological evaluation of 2-aroylbenzofurans, rugchalcones A, B and their derivatives as potent anti-inflammatory agents
Seo, Young Hwa,Damodar, Kongara,Kim, Jin-Kyung,Jun, Jong-Gab
supporting information, p. 1521 - 1524 (2016/07/29)
An efficient synthesis of 2-aroylbenzofurans, rugchalcones A, B and their derivatives was accomplished in excellent yields by the Rap–Stoermer reaction between substituted salicylaldehydes and phenacyl bromides. Later their anti-inflammatory effects were evaluated in lipopolysaccharide (LPS)-induced RAW-264.7 macrophages. The compounds were exhibited exceptional potency against inflammatory mediated NO production with no cytotoxicity at 10?μM concentration and IC50values are found in the range from 0.75 to 13.27?μM. Among the 2-aroylbenzofurans prepared in this study, compounds 4 (99.6%; IC50?=?0.57), rugchalcone B (2) (99.3%; IC50?=?4.13), 7 (96.8%; IC50?=?1.90) and 8 (74.3%; IC50?=?0.99) were showed the maximum inhibitory activity. This study suggests that compounds 2, 4, 7 and 8 which are having 4-hydroxyphenyl group and/or hydroxy (–OH) group at 5- and/or 6-position of benzofuran motif could be considered as a promising scaffolds for the further development of iNOS inhibitors for potential anti-inflammatory applications.
Platinum(II) Complexes with O,S Bidentate Ligands: Biophysical Characterization, Antiproliferative Activity, and Crystallographic Evidence of Protein Binding
Mügge, Carolin,Marzo, Tiziano,Massai, Lara,Hildebrandt, Jana,Ferraro, Giarita,Rivera-Fuentes, Pablo,Metzler-Nolte, Nils,Merlino, Antonello,Messori, Luigi,Weigand, Wolfgang
, p. 8560 - 8570 (2015/09/21)
We recently characterized a series of novel platinum(II) compounds bearing a conserved O,S binding moiety as a bifunctional ligand and evaluated their solution behavior and antiproliferative properties in vitro against a representative cancer cell line. O
Pyrazole-5-carboxamides, novel inhibitors of receptor for advanced glycation end products (RAGE)
Han, Young Taek,Kim, Kyeojin,Choi, Gyeong-In,An, Hongchan,Son, Dohyun,Kim, Hee,Ha, Hee-Jin,Son, Jun-Hyeng,Chung, Suk-Jae,Park, Hyun-Ju,Lee, Jeewoo,Suh, Young-Ger
, p. 128 - 142 (2014/05/06)
In an effort to develop novel inhibitors of receptor for advanced glycation end products (RAGE) for the treatment of Alzheimer's disease, a series of pyrazole-5-carboxamides were designed, synthesized and biologically evaluated. Analyses of the extensive
Environmentally benign deprotection of dithioacetals using 30% hydrogen peroxide catalyzed by Fe(acac)3 and sodium iodide
Kirihara, Masayuki,Suzuki, Satoshi,Ishizuka, Yuki,Yamazaki, Kento,Matsushima, Ryoji,Suzuki, Takaya,Iwai, Toshiaki
, p. 5477 - 5480 (2013/09/23)
The reaction of dithioacetals with 30% hydrogen peroxide in the presence of catalytic amounts of iron(III) acetylacetonate and sodium iodide efficiently produced the corresponding carbonyl compounds in high yields.
