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- Title
Discovery of a series of novel phenylpiperazine derivatives as EGFR TK inhibitors.
- Authors
Sun, Juan; Wang, Xin-Yi; Lv, Peng-Cheng; Zhu, Hai-Liang
- Abstract
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.
- Subjects
EPIDERMAL growth factor receptors; CELLULAR signal transduction; PIPERAZINE; CELL culture; TUMOR growth
- Publication
Scientific Reports, 2015, p13934
- ISSN
2045-2322
- Publication type
Article
- DOI
10.1038/srep13934