880771-40-4Relevant 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 (2018/03/05)
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
AZA-TANSHINONE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE IN THERAPY
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Page/Page column 64; 65, (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
A Palladium(II)-Catalyzed C-H Activation Cascade Sequence for Polyheterocycle Formation
Cooper, Stephen P.,Booker-Milburn, Kevin I.
, p. 6496 - 6500 (2015/06/02)
Polyheterocycles are found in many natural products and are useful moieties in functional materials and drug design. As part of a program towards the synthesis of Stemona alkaloids, a novel palladium(II)-catalyzed C-H activation strategy for the construction of such systems has been developed. Starting from simple 1,3-dienyl-substituted heterocycles, a large range of polycyclic systems containing pyrrole, indole, furan and thiophene moieties can be synthesized in a single step. Don't overdo it: A palladium(II)-catalyzed C-H activation cascade sequence for the synthesis of polyheterocycles is reported. Aromatization of the initially formed dihydro species occurred with a quinone oxidant. In some cases the use of one equivalent of the oxidant enabled isolation of the dihydro species as a single isomer (see scheme; X=NMe, O, S).
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.
body text, 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.
A concise synthesis of novel naphtho[a]carbazoles and benzo[c]carbazoles
Pathak, Rakhi,Nhlapo, Johanna M.,Govender, Sameshnee,Michael, Joseph P.,Van Otterlo, Willem A. L.,De Koning, Charles B.
, p. 2820 - 2830 (2007/10/03)
Starting from simple indole precursors the synthesis of naphtho[a]carbazoles and benzo[c]carbazoles is described. Key steps include the use of the Suzuki-Miyaura reaction to afford 2- or 3-aryl substituted indoles, as well as a potassium t-butoxide and light assisted aromatic ring-forming reaction.
