18073-21-7Relevant academic research and scientific papers
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
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.
Efficient microwave-assisted synthesis of ellipticine through N-(1,4-dimethyl-9h-carbazol-3-ylmethyl)-n-tosylaminoacetaldehyde diethyl acetal
Lee, Hsueh-Yun,Chen, Grace Shiahuy,Chen, Chien-Shu,Cherna, Ji-Wang
scheme or table, p. 454 - 458 (2010/06/19)
The long-lasting problematic low yield in the D-ring cyclization of ellipticine (1a) was dramatically improved through N-(1,4-dimethylcarbazol-3- ylmethyl)-N-tosylaminoacetaldehyde diethyl acetal with microwave irradiation. The overall yield of 1a starting from indole was significantly increased by 25-fold. This new approach is superior to reported methods in yields and, reaction time, and it provides efficient access to a broad spectrum of ellipticine derivatives.
