18028-57-4Relevant academic research and scientific papers
Identification of Lead Compounds as Inhibitors of STAT3: Design, Synthesis and Bioactivity
Botta, Antonio,Sirignano, Esther,Popolo, Ada,Saturnino, Carmela,Terracciano, Stefania,Foglia, Antonio,Sinicropi, Maria Stefania,Longo, Pasquale,Di Micco, Simone
, p. 689 - 697 (2015)
STAT3 belongs to the signal transducers and activators of transcription (STAT) family. It has been demonstrated that STAT3 is constitutively activated in many tumors, playing a role in carcinogenesis and tumor progression. For this reason, it has being co
Simple method for preparing ellipticine or substituted ellipticine
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Paragraph 0050-0053, (2020/05/14)
The invention relates to a synthesis process for preparing ellipticine. Ellipticine is obtained through six steps of reaction and three steps of crystallization separation, the target product total yield is high, column chromatography separation is not needed for an intermediate product and the target product, and the method is particularly suitable for large-scale preparation.
Design, synthesis, DNA binding studies and evaluation of anticancer potential of novel substituted biscarbazole derivatives against human glioma U87 MG cell line
Kumar, Nitin,Lal, Neetika,Nemaysh, Vishal,Luthra, Pratibha Mehta
, (2020/06/04)
In this research paper, we report the design and synthesis of novel substituted biscarbazole derivatives which were characterized by 1H and 13C NMR, high resolution mass spectroscopy (HRMS). The SAR study of the compounds is reported
The Hairpin Form of r(G4C2)exp in c9ALS/FTD Is Repeat-Associated Non-ATG Translated and a Target for Bioactive Small Molecules
Wang, Zi-Fu,Ursu, Andrei,Childs-Disney, Jessica L.,Guertler, Rea,Yang, Wang-Yong,Bernat, Viachaslau,Rzuczek, Suzanne G.,Fuerst, Rita,Zhang, Yong-Jie,Gendron, Tania F.,Yildirim, Ilyas,Dwyer, Brendan G.,Rice, Joseph E.,Petrucelli, Leonard,Disney, Matthew D.
, p. 179 - 12,190 (2019/02/19)
The most common genetic cause of amyotrophic lateral sclerosis (ALS) and frontotemporal dementia (FTD) is an expanded G4C2 repeat [(G4C2)exp] in C9ORF72. ALS/FTD-associated toxicity has been traced to
An efficient synthesis of (±) 4-hydroxy-9-methoxy-5,11-dimethyl-6H-1,2,3,4-tetrahydro-benzo [b] carbazole
Bengaouer, Mohamed Larbi,Boukhari, Abbes
, p. 1532 - 1540 (2017/11/10)
In this study, new tetracyclic compounds similar to benzo[b]carbazole have been synthesized. Their structures have been characterized by IR, 1H and 13C NMR, mass spectral and CHN analysis, and correspond to 4-hydroxy-9-methoxy-5,11-d
Synthesis and biological evaluation of new N-alkylcarbazole derivatives as STAT3 inhibitors: Preliminary study
Saturnino, Carmela,Palladino, Chiara,Napoli, Mariagrazia,Sinicropi, Maria Stefania,Botta, Antonio,Sala, Marina,Carcereri De Prati, Alessandra,Novellino, Ettore,Suzuki, Hisanori
, p. 112 - 119 (2013/04/10)
The signalling pathway of Janus tyrosine Kinases-Signal Transducers and Activators of Transcription (JAK-STAT) is activated by a number of cytokines, hormones (GH, erythropoietin and prolactin), and growth factors. JAK-STAT signalling is involved in regul
Antiproliferative activity of some 1,4-dimethylcarbazoles on cells that express estrogen receptors: Part i
Caruso, Anna,Chimento, Adele,El-Kashef, Hussein,Lancelot, Jean-Charles,Panno, Antonella,Pezzi, Vincenzo,Saturnino, Carmela,Sinicropi, Maria Stefania,Sirianni, Rosa,Rault, Sylvain
body text, p. 609 - 613 (2012/09/22)
Several 9H-carbazole derivatives are used for various pharmacological applications. Many of these compounds demonstrated cytotoxic and anticancer activities. In this work, we have investigated the cytotoxic activity of some substituted carbazoles against
Ellipticines and 9-acridinylamines as inhibitors of d-alanine:d-alanine ligase
Vehar, Bla?,Hrast, Martina,Kova?, Andreja,Konc, Janez,Mariner, Katherine,Chopra, Ian,O'Neill, Alex,Jane?i?, Du?anka,Gobec, Stanislav
experimental part, p. 5137 - 5146 (2011/10/04)
d-Alanine:d-alanine ligase (Ddl), an intracellular bacterial enzyme essential for cell wall biosynthesis, is an attractive target for development of novel antimicrobial drugs. This study focused on an extensive evaluation of two families of Ddl inhibitors encountered in our previous research. New members of both families were obtained through similarity search and synthesis. Ellipticines and 9-acridinylamines were both found to possess inhibitory activity against Ddl from Escherichia coli and antimicrobial activity against E. coli and Staphylococcus aureus. Ellipticines with a quaternary methylpyridinium moiety were the most potent among all studied compounds, with MIC values as low as 2 mg/L in strains with intact efflux mechanisms. Antimicrobial activity of the studied compounds was connected to membrane damage, making their development as antibacterial drug candidates unlikely unless analogues devoid of this nonspecific effect can be discovered.
Microwave-assisted solid-acid-catalyzed friedel-crafts alkylation and electrophilic annulation of indoles using alcohols as alkylating agents
Kulkarni, Aditya,Quang, Phong,Toeroek, Bela
experimental part, p. 4010 - 4014 (2010/04/02)
Alcohols are considered environmentally benign alkylating agents since the only by-product generated in their reactions is water. Herein, we report a microwave-assisted Friedel-Crafts alkylation and electrophilic annulation of indoles using alcohols as al
Solvent-free solid acid-catalyzed electrophilic annelations: A new green approach for the synthesis of substituted five-membered N-heterocycles
Abid, Mohammed,Spaeth, Andrew,Toeroek, Bela
, p. 2191 - 2196 (2007/10/03)
An effective microwave-induced, solid acid-catalyzed, environmentally benign synthesis of substituted pyrroles, indoles and carbazoles under solvent-free conditions is described. The new synthetic methodology is based on the use of a considerably strong solid acid, K-10 montmorillonite. Both the cyclialkylation of amines and annelation of pyrroles and indoles have been completed within minutes and provided excellent (75-98%) yields with practically 100% selectivity.
