848176-65-8Relevant academic research and scientific papers
2-Arylquinolines as novel anticancer agents with dual EGFR/FAK kinase inhibitory activity: synthesis, biological evaluation, and molecular modelling insights
Elbadawi, Mostafa M.,Eldehna, Wagdy M.,Abd El-Hafeez, Amer Ali,Somaa, Warda R.,Albohy, Amgad,Al-Rashood, Sara T.,Agama, Keli K.,Elkaeed, Eslam B.,Ghosh, Pradipta,Pommier, Yves,Abe, Manabu
, p. 349 - 372 (2021/12/24)
In this study, different assortments of 2-arylquinolines and 2,6-diarylquinolines have been developed. Recently, we have developed a new series of 6,7-dimethoxy-4-alkoxy-2-arylquinolines as Topoisomerase I (TOP1) inhibitors with potent anticancer activity. Utilising the SAR outputs from this study, we tried to enhance anticancer and TOP1 inhibitory activities. Though target quinolines demonstrated potent antiproliferative effect, specifically against colorectal cancer DLD-1 and HCT-116, they showed weak TOP1 inhibition which may be attributable to their non-coplanarity. Thereafter, screening against kinase panel revealed their dual inhibitory activity against EGFR and FAK. Quinolines 6f, 6h, 6i, and 20f were the most potent EGFR inhibitors (IC50s = 25.39, 20.15, 22.36, and 24.81 nM, respectively). Meanwhile, quinolines 6f, 6h, 6i, 16d, and 20f exerted the best FAK inhibition (IC50s = 22.68, 14.25, 18.36, 17.36, and 15.36 nM, respectively). Finally, molecular modelling was employed to justify the promising EGFR/FAK inhibition. The study outcomes afforded the first reported quinolines with potent EGFR/FAK dual inhibition.
4-aminoquinoline compound, and preparation method and application thereof
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Paragraph 0032-0037, (2019/11/12)
The invention discloses a 4-aminoquinoline compound, and a preparation method and application thereof. The second site of the 4-aminoquinoline compound is replaced by cyclic R-base, the 4-aminoquinoline compound is obtained by 4-step reaction of anthranil
N-Bu4NI-catalyzed selective dual amination of sp3 C-H bonds: Oxidative domino synthesis of imidazo[1,5-c]quinazolines on a gram-scale
Zhao, Dan,Wang, Teng,Shen, Qi,Li, Jian-Xin
supporting information, p. 4302 - 4304 (2014/04/17)
An n-Bu4NI catalyzed domino reaction that involves selective dual amination of sp3 C-H bonds has been developed. The protocol affords a facile and efficient approach to the synthesis of imidazo[1,5-c] quinazolines under mild conditions.
