24522-20-1Relevant academic research and scientific papers
Discovery of 8-amino-substituted 2-phenyl-2,7-naphthyridinone derivatives as new c-Kit/VEGFR-2 kinase inhibitors
Sun, Haiyan,Zhuo, Linsheng,Dong, Huan,Huang, Wei,She, Nengfang
, (2019)
The 2,7-naphthyridone scaffold has been proposed as a novel lead structure ofMETinhibitors by our group. To broaden the application of this new scaffold, a series of 8-amino-substituted 2-phenyl-2,7-naphthyridin-1(2H)-one derivatives were designed and synthesized. Preliminary biological screening resulted in the discovery of a new lead of c-Kit and VEGFR-2 kinase inhibitors. Compound 9k exhibited excellent c-Kit inhibitory activity, with an IC50 value of 8.5 nM, i.e., it is 38.8-fold more potent than compound 3 (IC50 of 329.6 nM). Moreover, the compounds 10l and 10r exhibited good VEGFR-2 inhibitory activity, with IC50 values of 56.5 and 31.7 nM, respectively, i.e., they are 5.0-8.8-fold more potent than compound 3 (IC50 of 279.9 nM). Molecular docking experiments provided further insight into the binding interactions of the new lead compounds with c-Kit and VEGFR-2 kinase. In this study, an 8-amino-substituted 2-phenyl-2,7-naphthyridin-1(2H)-one scaffold was identified as the new lead structure of c-Kit and VEGFR-2 kinase inhibitors.
2,7-naphthyridinone-based MET kinase inhibitors: A promising novel scaffold for antitumor drug development
Zhuo, Lin-Sheng,Xu, Hong-Chuang,Wang, Ming-Shu,Zhao, Xing-E.,Ming, Zhi-Hui,Zhu, Xiao-Lei,Huang, Wei,Yang, Guang-Fu
, p. 705 - 714 (2019)
As part of our effort to develop new molecular targeted antitumor drug, a novel 2,7-naphthyridone-based MET kinase inhibitor, 8-((4-((2-amino-3-chloropyridin-4-yl)oxy)- 3-fluorophenyl)amino)-2-(4-fluorophenyl)-2,7-naphthyridin-1(2H)-one (13f), was identif
Synthesis of N-substituted 4,6-dimethyl-3-cyano-2-pyridones under microwave irradiation
Mijin, Du?an,Marinkovi?, Aleksandar
, p. 193 - 198 (2007/10/03)
N-substituted 4,6-dimethyl-3-cyano-2-pyridones have been prepared from acetylacetone, N-substituted cyanoacetamide, and pyperidine as catalyst under microwave irradiation without solvent. The rapid and simple method produced pure products in high yields. Copyright Taylor & Francis LLC.
Cyanoacetanilides intermediates in heterocyclic synthesis. Part 1: A facile synthesis of polysubstituted and condensed pyridones
Ammar,El-Sharief,Mohamed,Salem,Al-Sehemi,El-Gaby
, p. 975 - 981 (2007/10/03)
Polysubstituted pyridone derivatives were obtained through interaction of cyanoacetanilides with different reagents such as chalcones, 1,1,3-tricyano-2-aminopropene, and arylidenemalononitrile and acetyl-acetone.
