Ontology highlight
ABSTRACT:
SUBMITTER: Wang C
PROVIDER: S-EPMC6282443 | biostudies-literature | 2019 Dec
REPOSITORIES: biostudies-literature
Journal of enzyme inhibition and medicinal chemistry 20191201 1
A series of quinazoline derivatives with benzylidene hydrazine carboxamide were designed and synthesised as EGFR inhibitors. Most compounds exhibited exceptional anti-proliferative activity against A549, HepG2, MCF-7 and H1975 cells. Furthermore, six compounds demonstrated excellent inhibition activity against EGFR<sup>WT</sup> with the IC<sub>50</sub> value both less than 2 nM. Among the six compounds, 44 exhibited the strongest activity (0.4 nM) and potently inhibited EGFR<sup>L858R/T790M</sup ...[more]