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Article

Design, synthesis and antitumor activity of novel thiophene-pyrimidine derivatives as EGFR inhibitors overcoming T790M and L858R/T790M mutations.

European journal of medicinal chemistry - 1 Oct 2020

Xiao Zhen, Zhou Zhihui, Chu Cilong, Zhang Qian, Zhou Lingjia, Yang Zunhua, Li Xin, Yu Liying, Zheng Pengwu, Xu Shan, Zhu Wufu

Abstract excerpt

Five series of novel thiophene-pyrimidine derivatives (9a-h, 10a-f, 11a-f, 12a-f, 13a-f) have been synthesized and tested for their anti-proliferative activity against several cancer cell lines in which EGF is highly expressed. Most of the target compounds showed excellent activity against one or more cancer cell lines. The most promising compound 13a, of which IC50 values on of cell lines A549 and A431...

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Identifiers

PMID: 32679450
DOI: 10.1016/j.ejmech.2020.112511

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