58914-17-3

Upstream product

• 38875-53-5 5-bromo-pyridine-2,3-diamine 
• 1074-12-0 phenylglyoxal hydrate 

Downstream Products

• 139436-71-8 3-phenyl-8-pyrrolidino-5-azaquinoxaline 
• 139436-73-0 3-phenyl-8-morpholino-5-azaquinoxaline 
• 117902-04-2 7-bromo-5,6-dihydro-3-phenylpyrido<2,3-b>pyrazine 
• 117902-05-3 7-bromo-1,2-dihydro-3-phenylpyrido<2,3-b>pyrazine 
• 58914-16-2 phenyl-3 pyrido<2,3-b>pyrazine 
• 139436-72-9 3-phenyl-8-piperidine-5-azaquinoxaline 

Relevant academic research and scientific papers

Preparation of pyrido [2,3-b] pyrazine ring system via regioselective condensation reaction

The pyrido[2,3-b]pyrazine core structure can be found in several molecules that express biological activity. We have previously published a series of these compounds that showed erlotinib-resistant tumor inhibitor potential. The common way of their synthe

PYRIDOPYRAZINES AS ANTICANCER AGENTS

The present invention relates to pyridopyrazine derivatives and solvates, hydrates and pharmaceutically acceptable salts thereof, the use of them in the prevention and/or the treatment of cancer diseases, as well as pharmaceutical compositions containing at least one of them as pharmaceutically active agent(s) together with pharmaceutically acceptable carrier, excipient and/or diluents, especially for the prevention and/or treatment of cancer diseases.˙

Synthesis and biological evaluation of novel pyrido[2,3-b]pyrazines inhibiting both erlotinib-sensitive and erlotinib-resistant cell lines

A series of novel pyrido[2,3-b]pyrazines were synthesized as potential antitumor agents for erlotinib-resistant tumors. Known signal inhibitor compounds from our Nested Chemical Library were tested in phenotypic assays on erlotinib-sensitive PC9 and erlotinib-resistant PC9-ER cell lines to find a compound class to be active on erlotinib resistant cell lines. Based on the screening data, novel pyrido[2,3-b]pyrazines were designed and synthesized. The effect of the substituent position of the heteroaromatic moiety in position 7 and the importance of unsubstituted position 2 of the pyridopyrazine core were explored. Compound 7n had an IC50 value of 0.09 μM for the inhibition of PC9 and 0.15 μM for the inhibition of PC9-ER. We found that some lead compounds of these structures overcome erlotinib-resistance which might become promising drug candidates to fight against NSCLC with EGFR T790M mutation. The signaling network(s) involved in the mechanism(s) of action of these novel compounds in overcoming erlotinib resistance remain to be elucidated.