1566577-85-2

Upstream product

• 1566577-39-6 1-(2,6-dimethylphenyl)pyrimidine-2,4,6-trione 
• 2990-03-6 1-(2,6-dimethylphenyl)urea 
• 87-62-7 2,6-dimethylaniline 
• 960299-66-5 4-(2-fluoro-4-nitrophenoxy)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline 
• 1061610-61-4 4-chloro-6-methoxy-7-(3-(4-methylpiperazin-1-yl)-propoxy)quinoline 
• 1394166-09-6 6-methyloxy-7-(4-(3-chloropropoxy))-4-4-hydroxyquinoline 
• 1449763-02-3 1-(4-(3-chloropropoxy)-5-methoxy-2-nitrophenyl)-3-(dimethylamino)propyl-2-en-1-one 
• 1160707-44-7 1-[4-(3-chloropropoxy)-5-methoxy-2-nitrophenyl]ethan-1-one 
• 58113-30-7 4-(3-chloropropoxy)-3-methoxyacetophenone 
• 498-02-2 1-(3-methoxy-4-hydroxyphenyl)ethanone 
• 960299-67-6 3-fluoro-4-{6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinolin-4-yloxy}phenylamine 
• 1566577-45-4 (E)-5-((dimethylamino)methylene)-1-(2,6-dimethylphenyl)pyrimidine-2,4,6-trione 

Relevant academic research and scientific papers

Pyrimidones including six hydrogens quinoline compound and its preparation method and application

The invention relates to a quinolines compound containing hexahydropyrimidone, which is represented by a formula I, as well as pharmaceutically acceptable configurational isomers, salts, hydrates, solvates and prodrugs thereof. According to the quinolines compound, substituent groups R1, R2, R3, X, Y, Z and n have definitions given in the specification. The invention further relates to the compound of the formula I and the configurational isomers which have a very strong effect of inhibiting c-Met kinase, further relates to an application of the compounds and the pharmaceutically acceptable salts, hydrates, solvates or prodrugs in preparing a medicine for treating diseases caused by hydrates high expression of the c-Met kinase, and particularly relates to an application of a medicine for preparing a medicine for treating and/or preventing cancers.

Discovery of novel 6,7-disubstituted-4-phenoxyquinoline derivatives bearing 5-(aminomethylene)pyrimidine-2,4,6-trione moiety as c-Met kinase inhibitors

A series of novel quinoline derivatives bearing 5-(aminomethylene) pyrimidine-2,4,6-trione moiety were designed, synthesized, and evaluated for their c-Met kinase inhibitory activities and antiproliferative activities against 5 cancer cell lines (HT-29, H460, MKN-45, A549, and U87MG) in vitro. Most compounds showed moderate to excellent potency, with the most promising analogue 45 (c-Met half-maximal inhibitory concentration [IC50] = 1.15 nM) showing high selectivity versus 5 other tyrosine kinases, VEGFR-2, Flt-3, PDGFR-β, c-Kit, and EGFR. Structure-activity relationship studies indicated that electron-donating groups on the phenyl ring at the 3-position of pyrimidine-2,4,6-trione were required to increase the electron density on the 5-(aminomethylene)pyrimidine-2,4,6-trione moiety.