Article
New acrylamide-substituted quinazoline derivatives with enhanced potency for the treatment of EGFR T790M-mutant non-small-cell lung cancers.
Bioorganic chemistry - 1 Apr 2018
Liu Zhuo, Wang Luhong, Feng Min, Yi Yuanyuan, Zhang Wenhan, Liu Wenjuan, Li Lei, Liu Zhihao, Li Yanxia, Ma Xiaodong
Abstract excerpt
A new class of acrylamide-substituted quinazoline derivatives with enhanced inhibitory activity against mutant EGFR T790M enzyme were synthesized. Among them, compound 10b displayed the strongest inhibitory potency to block the phosphorylation of the EGFR T790M enzyme, with an IC50 value of 4.3 nM. Compared with the lead compound gefitinib, compound 10b significantly strengthened the activity against EGFR T790M...
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