Kekesi, Laszlo published the artcileSynthesis and biological evaluation of novel pyrido[2,3-b]pyrazines inhibiting both erlotinib-sensitive and erlotinib-resistant cell lines, SDS of cas: 371766-08-4, the publication is Bioorganic & Medicinal Chemistry Letters (2013), 23(22), 6152-6155, database is CAplus and MEDLINE.
A series of novel pyrido[2,3-b]pyrazines I [R1 = H, Ph, 4-MeC6H4, etc.; R2 = H, Ph, 2-thienyl, etc.; R3 = pyridin-3-yl, quinolin-3-yl; indol-4-yl, etc.] were synthesized as potential antitumor agents for erlotinib-resistant tumors. Known signal inhibitor compounds from the Nested Chem. 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 I [R1R2 = 1,4-benzodioxan-6-yl; R3 = indol-5-yl] had an IC50 value of 0.09 μM for the inhibition of PC9 and 0.15 μM for the inhibition of PC9-ER. The authors 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.
Bioorganic & Medicinal Chemistry Letters published new progress about 371766-08-4. 371766-08-4 belongs to isoquinoline, auxiliary class Isoquinoline,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is Isoquinolin-5-ylboronic acid, and the molecular formula is C9H8BNO2, SDS of cas: 371766-08-4.
Referemce:
https://en.wikipedia.org/wiki/Isoquinoline,
Isoquinoline | C9H7N – PubChem