1190709-19-3Relevant academic research and scientific papers
Interfering with HuR-RNA Interaction: Design, Synthesis and Biological Characterization of Tanshinone Mimics as Novel, Effective HuR Inhibitors
Manzoni, Leonardo,Zucal, Chiara,Maio, Danilo Di,D'Agostino, Vito G.,Thongon, Natthakan,Bonomo, Isabelle,Lal, Preet,Miceli, Marco,Baj, Vanessa,Brambilla, Marta,Cerofolini, Linda,Elezgarai, Saioa,Biasini, Emiliano,Luchinat, Claudio,Novellino, Ettore,Fragai, Marco,Marinelli, Luciana,Provenzani, Alessandro,Seneci, Pierfausto
, p. 1483 - 1498 (2018)
The human antigen R (HuR) is an RNA-binding protein known to modulate the expression of target mRNA coding for proteins involved in inflammation, tumorigenesis, and stress responses and is a valuable drug target. We previously found that dihydrotanshinone
Synthesis method of novel HuR inhibitor 1-benzenesulfonyl-3-phenylindole-4, 5-diketone
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, (2021/08/14)
The invention discloses a synthesis method of a novel HuR inhibitor 1-benzenesulfonyl-3-phenylindole-4, 5-diketone, 5-methoxyindole is used as an initial raw material, C-3 site of 5-methoxyindole and aryl halide region are subjected to selective arylation, then benzenesulfonyl chloride is used for treatment to prepare 1-benzenesulfonyl-3-phenylindole, and finally, by carrying out demethylation and oxidation, a target product, namely the 1-benzenesulfonyl-3-phenylindole-4, 5-diketone is synthesized . The synthesis method has the advantages of simple synthesis route, short reaction time, simplicity in operation and the like.
AZA-TANSHINONE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE IN THERAPY
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Page/Page column 65; 66, (2018/01/20)
Object of the present invention are new aza-tanshinone derivatives, a method for their preparation and their use in therapy, particularly, but not limited to, as anti? tumor agents and anti-inflammatories. The invention comprises also the pharmaceutical c
Regiocontrolled aerobic oxidative coupling of indoles and benzene using Pd catalysts with 4,5-diazafluorene ligands
Campbell, Alison N.,Meyer, Eric B.,Stahl, Shannon S.
, p. 10257 - 10259 (2011/10/19)
Palladium-catalyzed aerobic oxidative cross-couplings of indoles and benzene have been achieved by using 4,5-diazafluorene derivatives as ancillary ligands. Proper choice of the neutral and anionic ligands enables control over the reaction regioselectivit
The synthesis of 2- and 3-aryl indoles and 1,3,4,5-tetrahydropyrano[4,3-b]indoles and their antibacterial and antifungal activity
Leboho, Tlabo C.,Michael, Joseph P.,van Otterlo, Willem A.L.,van Vuuren, Sandy F.,de Koning, Charles B.
scheme or table, p. 4948 - 4951 (2009/12/24)
A series of 2- and 3-aryl substituted indoles and two 1,3,4,5-tetrahydropyrano[4,3-b]indoles were synthesized from indole and 5-methoxyindole. The 2-aryl indoles were synthesized from the 1-(phenylsulfonyl)indole derivatives using magnesiation followed by iodination. The 2-iodinated compounds were then subjected to Suzuki-Miyaura reactions. In addition, the 3-aryl indoles were made from the corresponding 3-bromoindoles using Suzuki-Miyaura reactions. The 1,3,4,5-tetrahydropyrano[4,3-b]indoles were also synthesized from 1-(phenylsulfonyl)indole by magnesiation followed by treatment with allylbromide. The product was then converted into [2-allyl-1-(phenylsulfonyl)-1H-indol-3-yl]methanol which upon exposure to Hg(OAc)2 and NaBH4 afforded tetrahydropyrano[4,3-b]indoles. A number of the 2- and 3-aryl indoles displayed noteworthy antimicrobial activity, with compound 13a displaying the most significant activity (3.9 μg/mL) against the Gram-positive micro-organism Bacillus cereus.
