文章基本信息

标题：Discovery of a series of novel phenylpiperazine derivatives as EGFR TK inhibitors
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作者：Juan Sun ; Xin-Yi Wang ; Peng-Cheng Lv 等
期刊名称：Scientific Reports
电子版ISSN：2045-2322
出版年度：2015
卷号：5
DOI：10.1038/srep13934
出版社：Springer Nature
摘要：Human epidermal growth factor receptor (EGFR) is an important drug target that plays a fundamental role in signal transduction pathways in oncology. We report herein the discovery of a novel class of phenylpiperazine derivatives with improved potency toward EGFR. The biological activity of compound 3p as inhibitor of EGFR was further investigated both in vitro and in vivo . Notably, compound 3p exhibited an IC₅₀ in the nanomolar range in A549 cell cultures and induced a cessation of tumor growth with no toxicity, as determined by loss of body weight and death of treated mice. Compoutational docking studies also showed that compound 3p has interaction with EGFR key residues in the active site.