Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. In an article, author is Wang, Ming-Shu, once mentioned the application of 39156-41-7, Name is 4-Methoxybenzene-1,3-diamine sulfate, molecular formula is C7H12N2O5S, molecular weight is 236.2456, MDL number is MFCD00012978, category is naphthyridine. Now introduce a scientific discovery about this category, Product Details of 39156-41-7.
Synthesis and biological evaluation of new MET inhibitors with 1,6-naphthyridinone scaffold
A potent and novel MET inhibitor, 5-((4((2-amino-3-chloropyridin-4-yl)oxy)-3-fluorophenyl)amino)-3-(4-fluorophenyl)-1,6-naphthyridin-4(1H)-ones (8), was designed and synthesized via a scaffold-hopping strategy of a 2,7-naphthyridinone MET kinase inhibitor 7. Lead compound 8 had good potency (IC50 of 9.8 nM), but unfavorable pharmacokinetic profiles (F = 12%, CL = 5.0 L/h/kg). Systematic structural optimization of compound 8 resulted in 9g (MET, IC50 – of 9.8 nM) with a comparable MET potency to that of compound 2 and a favorable pharmacokinetic profile (F= 63%, CL = 0.12 L/h/kg). Further study of the derivatization of N(1) amine group of 9g led to the discovery of 23a with good MET potency (IC50 of 7.1 nM), promising VEGFR-2 selectivity (3226-fold), and a markedly drug-likeness improvement (F= 57.7%, CL = 0.02 L/h/kg). The excellent VEGFR-2 selectivity and favorable drug-likeness of 23g suggest that the 1,6-naphthyridine moiety could be used as a new scaffold for kinase inhibitor discovery. (C) 2019 Elsevier Masson SAS. All rights reserved.
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Reference:
1,8-Naphthyridine – Wikipedia,
,1,8-Naphthyridine | C8H6N2 – PubChem