153436-72-7Relevant articles and documents
4-amino-quinazoline derivatives and antiviral composition comprising the same
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Paragraph 0094; 0098-0099; 0212; 0214-0215, (2021/04/13)
4 -amino - quinazoline (4-amino-quinazoline) derivatives or pharmaceutically acceptable salts thereof, processes for their preparation, and viral therapeutics containing them as active ingredients.
Identification of 4-anilino-6-aminoquinazoline derivatives as potential MERS-CoV inhibitors
Jang, Min Seong,Jin, Young-hee,Kim, Hyoung Rae,Kim, Seungtaek,Kwon, Sunoh,Lee, Jihye,Lee, Jun Young,Park, Chul Min,Shin, Young Sup,Song, Jong Hwan
, (2020/08/19)
New therapies for treating coronaviruses are urgently needed. A series of 4-anilino-6-aminoquinazoline derivatives were synthesized and evaluated to show high anti-MERS-CoV activities. N4-(3-Chloro-4-fluorophenyl)-N6-(3-methoxybenzyl
First Bispecific Inhibitors of the Epidermal Growth Factor Receptor Kinase and the NF-κB Activity As Novel Anticancer Agents
Hamed, Mostafa M.,Darwish, Sarah S.,Herrmann, Jennifer,Abadi, Ashraf H.,Engel, Matthias
supporting information, p. 2853 - 2868 (2017/04/21)
The activation of the NF-κB transcription factor is a major adaptive response induced upon treatment with EGFR kinase inhibitors, leading to the emergence of resistance in nonsmall cell lung cancer and other tumor types. To suppress this survival mechanism, we developed new thiourea quinazoline derivatives that are dual inhibitors of both EGFR kinase and the NF-κB activity. Optimization of the hit compound, identified in a NF-κB reporter gene assay, led to compound 9b, exhibiting a cellular IC50 for NF-κB inhibition of 0.3 μM while retaining a potent EGFR kinase inhibition (IC50 = 60 nM). The dual inhibitors showed a higher potency than gefitinib to inhibit cell growth of EGFR-overexpressing tumor cell lines in vitro and in a xenograft model in vivo, while no signs of toxicity were observed. An investigation of the molecular mechanism of NF-κB suppression revealed that the dual inhibitors depleted the transcriptional coactivator CREB-binding protein from the NF-κB complex in the nucleus.
