77987-49-6Relevant articles and documents
Design, physico-chemical characterization andin vitrobiological activity of organogold(iii) glycoconjugates
Pettenuzzo, Andrea,Vezzù, Keti,Di Paolo, Maria Luisa,Fotopoulou, Eirini,Marchiò, Luciano,Via, Lisa Dalla,Ronconi, Luca
supporting information, p. 8963 - 8979 (2021/07/02)
To develop new metal-based glycoconjugates as potential anticancer agents, four organometallic gold(iii)-dithiocarbamato glycoconjugates of the type [AuIII(2-Bnpy)(SSC-Inp-GlcN)](PF6) (2-Bnpy: 2-benzylpyridine; Inp: isonipecotic moie
Preparation method of N-(2-aminoethyl) morpholine
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Paragraph 0062-0064; 0073-0075, (2021/04/21)
The invention provides a preparation method of N-(2-aminoethyl) morpholine, which comprises the following steps: S1, adding ethanolamine into dichloromethane to fully dissolve, dropwise adding benzyl chloroformate into the solution, and reacting under alkaline conditions to generate an intermediate 1; S2, adding the intermediate 1 into dichloromethane, fully dissolving, dropwise adding 4toluenesulfonyl chloride, and reacting under an alkaline condition to generate an intermediate 2; S3, adding the intermediate 2 into acetonitrile to be fully dissolved, adding morpholine into the acetonitrile to generate an intermediate 3, wherein the structural formula of the intermediate 3 is shown as the following formula (3); and S4, adding the intermediate 3 into methanol, fully dissolving, and carrying out a catalytic hydrogenation reaction under the action of a catalyst to generate N-(2-aminoethyl)morpholine. According to the N-(2-aminoethyl)morpholine preparation method provided by the embodiment of the invention, the raw materials used in the reaction are cheap and easily available, the toxicity is low, the operation is simple and convenient, and the method has less three wastes and is more environment-friendly.
Oxyenamides as Versatile Building Blocks for a Highly Stereoselective One-Pot Synthesis of the 1,3-Diamino-2-ol-Scaffold Containing Three Continuous Stereocenters
Bolte, Michael,Grimmer, Jennifer,Kelm, Harald,Kramer, Philipp,Krieg, Sara-Cathrin,Manolikakes, Georg
supporting information, p. 23667 - 23671 (2021/09/30)
A highly diastereoselective one-pot synthesis of the 1,3-diamino-2-alcohol unit bearing three continuous stereocenters is described. This method utilizes 2-oxyenamides as a novel type of building block for the rapid assembly of the 1,3-diamine scaffold containing an additional stereogenic oxygen functionality at the C2 position. A stereoselective preparation of the required (Z)-oxyenamides is reported as well.
Interplay between a Foldamer Helix and a Macrocycle in a Foldarotaxane Architecture
Gauthier, Maxime,Koehler, Victor,Clavel, Caroline,Kauffmann, Brice,Huc, Ivan,Ferrand, Yann,Coutrot, Frédéric
supporting information, p. 8380 - 8384 (2021/03/16)
The design and synthesis of a novel rotaxane/foldaxane hybrid architecture is reported. The winding of an aromatic oligoamide helix host around a dumbbell-shaped thread-like guest, or axle, already surrounded by a macrocycle was evidenced by NMR spectrosc
PROCESS OF PREPARING ARACHIDONOYLETHANOLAMINE ANALOGUES
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Page/Page column 25, (2021/05/29)
The present application provides new processes for preparing arachidonoylethanolamine analogues. Intermediates useful for preparing the compounds are also provided.
Discovery of New Imidazo[2,1- b]thiazole Derivatives as Potent Pan-RAF Inhibitors with Promising in Vitro and in Vivo Anti-melanoma Activity
Abdel-Maksoud, Mohammed S.,El-Gamal, Mohammed I.,Lee, Bong S.,Gamal El-Din, Mahmoud M.,Jeon, Hong R.,Kwon, Dow,Ammar, Usama M.,Mersal, Karim I.,Ali, Eslam M. H.,Lee, Kyung-Tae,Yoo, Kyung Ho,Han, Dong Keun,Lee, Jae Kyun,Kim, Garam,Choi, Hong Seok,Kwon, Young Jik,Lee, Kwan Hyi,Oh, Chang Hyun
, p. 6877 - 6901 (2021/06/25)
BRAF is an important component of MAPK cascade. Mutation of BRAF, in particular V600E, leads to hyperactivation of the MAPK pathway and uncontrolled cellular growth. Resistance to selective inhibitors of mutated BRAF is a major obstacle against treatment of many cancer types. In this work, a series of new (imidazo[2,1-b]thiazol-5-yl)pyrimidine derivatives possessing a terminal sulfonamide moiety were synthesized. Pan-RAF inhibitory effect of the new series was investigated, and structure-activity relationship is discussed. Antiproliferative activity of the target compounds was tested against the NCI-60 cell line panel. The most active compounds were further tested to obtain their IC50 values against cancer cells. Compound 27c with terminal open chain sulfonamide and 38a with a cyclic sulfamide moiety showed the highest activity in enzymatic and cellular assay, and both compounds were able to inhibit phosphorylation of MEK and ERK. Compound 38a was selected for testing its in vivo activity against melanoma. Cellular and animal activities are reported.
OLEOYLETHANOLAMIDE COMPOUNDS
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Page/Page column 43, (2021/10/02)
The present application provides oleoylethanolamide compounds useful for treating a disease or disorder in a subject in need thereof. Pharmaceutical compositions comprising the compounds and methods of treating diseases or disorders are also provided.
PALMITOYLETHANOLAMIDE COMPOUNDS
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Page/Page column 43, (2021/10/02)
The present application provides palmitoylethanolamide compounds useful for treating a disease or disorder in a subject in need thereof. Pharmaceutical compositions comprising the compounds and methods of treating diseases or disorders are also provided.
Solution-Phase Synthesis of Backbone-Constrained Cationic Peptoid Hexamers with Antibacterial and Anti-Biofilm Activities
Charbonnel, Nicolas,Faure, Sophie,Forestier, Christiane,Roy, Olivier,Shyam, Radhe,Taillefumier, Claude
supporting information, p. 5813 - 5822 (2021/11/17)
Abstract: Submonomer synthesis in solution and block-coupling protocols were combined to prepare amphiphilic peptoid hexamers. The amphipathic character arises from the use of hydrophobic aliphatic tert-butyl side-chains imposing the cis-amide backbone co
Design, synthesis and anticancer profile of new 4-(1H-benzo[d]imidazol-1-yl)pyrimidin-2-amine-linked sulfonamide derivatives with V600EBRAF inhibitory effect
Abdel-Maksoud, Mohammed S.,Mohamed, Ahmed A. B.,Hassan, Rasha M.,Abdelgawad, Mohamed A.,Chilingaryan, Garri,Selim, Samy,Abdel-Bakky, Mohamed S.,Al-Sanea, Mohammad M.
, (2021/10/01)
A new series of 4-(1H-benzo[d]imidazol-1-yl)pyrimidin-2-amine linked sulfonamide derivatives 12a–n was designed and synthesized according to the structure of well-established V600EBRAF inhibitors. The terminal sulfonamide moiety was linked to the pyrimidine ring via either ethylamine or propylamine bridge. The designed series was tested at fixed concentration (1 μM) against V600EBRAF, finding that 12e, 12i and 12l exhibited the strongest inhibitory activity among all target compounds and 12l had the lowest IC50 of 0.49 μM. They were further screened on NCI 60 cancer cell lines to reveal that 12e showed the most significant growth inhibition against multiple cancer cell lines. Therefore, cell cycle analysis of 12e was conducted to investigate the effect on cell cycle progression. Finally, virtual docking studies was performed to gain insights for the plausible binding modes of vemurafenib, 12i, 12e and 12l.