Discovery of 8-amino-substituted 2-phenyl-2,7-naphthyridinone derivatives as new c-Kit/VEGFR-2 kinase inhibitors was written by Sun, Haiyan;Zhuo, Linsheng;Dong, Huan;Huang, Wei;She, Nengfang. And the article was included in Molecules in 2019.Category: isoquinoline This article mentions the following:
The 2,7-naphthyridone scaffold has been proposed as a novel lead structure of MET inhibitors 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 biol. 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 IC50values of 56.5 and 31.7 nM, resp., i.e., they are 5.0-8.8-fold more potent than compound 3 (IC50 of 279.9 nM). Mol. 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. In the experiment, the researchers used many compounds, for example, Isoquinolin-7-amine (cas: 23707-37-1Category: isoquinoline).
Isoquinolin-7-amine (cas: 23707-37-1) belongs to isoquinoline derivatives. Quinoline is a catabolite of tryptophan, the basic structure of some antihypertensive drugs, such as the peripheral vasodilators prazosin and doxazosin. The Pomeranz–Fritsch reaction provides a method for the preparation of isoquinoline. This reaction uses a benzaldehyde and aminoacetoaldehyde diethyl acetal, which in an acid medium react to form isoquinoline.Category: isoquinoline
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem