Article
Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFRT790M mutant cell lines.
European journal of medicinal chemistry - 5 Mar 2021
Zhao Lei, Fan Tingting, Shi Zhichao, Ding Chao, Zhang Cunlong, Yuan Zigao, Sun Qinsheng, Tan Chunyan, Chu Bizhu, Jiang Yuyang
Abstract excerpt
Acquired resistance leads to the failure of EGFR TKIs in NSCLC treatment. A novel series of hydroxamic acid-containing 4-aminoquinazoline derivatives as irreversible ErbB/HDAC multitargeted inhibitors for NSCLC therapy had been designed and synthesized, which displayed weak anti-proliferative activity in several EGFR wild-type cancer cell lines (NCI-H838, SK-BR-3, A549, A431) yet retained moderate activity to...
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