29079-97-8Relevant academic research and scientific papers
PROPENAMIDE THIOPHENE DERIVATIVES AS FLAVIVIRUS INHIBITORS AND THEIR USE
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Page/Page column 19; 20, (2017/07/06)
The present invention deals with new flavivirus inhibitors, compositions comprising said inhibitors and methods for the treatment of disorders related to a viral infection, such as a disease due to a flavivirus infection, comprising administering said inhibitors.
Discovery of novel 4-anilinoquinazoline derivatives as potent inhibitors of epidermal growth factor receptor with antitumor activity
Xu, Yun-Yun,Li, Si-Ning,Yu, Gao-Jian,Hu, Qing-Hua,Li, Huan-Qiu
, p. 6084 - 6091 (2013/09/23)
Two new series of new compounds containing a 6-amino-substituted group or 6-acrylamide-substituted group linked to a 4-anilinoquinazoline nucleus have been discovered as potential EGFR inhibitors. These compounds proved efficient effects on antiproliferative activity and EGFR-TK inhibitory activity. Especially, N6-((5-bromothiophen-2-yl)methyl)-N4-(3- chlorophenyl)quinazoline-4,6-diamine (5e), showed the most potent inhibitory activity (IC50 = 3.11 μM for Hep G2, IC50 = 0.82 μM for A549). The EGFR molecular docking model suggested that the new compound is nicely bound to the region of EGFR, and cell morphology by Hoechst stain experiment suggested that these compounds efficiently induced apoptosis of A549 cells.
Identification of 2-(4-pyridyl)thienopyridinones as GSK-3β inhibitors
Gentile, Gabriella,Bernasconi, Giovanni,Pozzan, Alfonso,Merlo, Giancarlo,Marzorati, Paola,Bamborough, Paul,Bax, Benjamin,Bridges, Angela,Brough, Caroline,Carter, Paul,Cutler, Geoffrey,Neu, Margarete,Takada, Mia
scheme or table, p. 4823 - 4827 (2011/09/21)
The discovery of a novel series of 2-(4-pyridyl)thienopyridinone GSK-3β inhibitors is reported. X-ray crystallography reveals its binding mode and enables rationalization of the SAR. The initial optimization of the template for improved cellular activity and predicted CNS penetration is also presented.
Heteroaryl-substituted carboxamides and use thereof for the stimulation of the expression of NO synthase
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Page/Page column 34-35, (2008/12/06)
The present invention relates to heteroaryl-substituted carboxamides of the formula I, in which Het, A, X, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxi
