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Evaluation of Novel N ‐(piperidine‐4‐yl)benzamide Derivatives as Potential Cell Cycle Inhibitors in HepG2 Cells
Author(s) -
Hou Jin,
Zhao Wei,
Huang ZhiNing,
Yang ShaoMei,
Wang LiJuan,
Jiang Yu,
Zhou ZhongShi,
Zheng ManYi,
Jiang JiLi,
Li ShanHua,
Li FuNan
Publication year - 2015
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12484
Subject(s) - benzamide , piperidine , chemistry , cell cycle , western blot , flow cytometry , cell cycle checkpoint , ic50 , cyclin b1 , stereochemistry , biochemistry , microbiology and biotechnology , cell , in vitro , biology , cyclin dependent kinase 1 , gene
In this study, a series of novel N ‐(piperidine‐4‐yl)benzamide derivatives was designed, synthesized, and evaluated for antitumor activity. Some compounds were found to have potent antitumor activity. In particular, compound 47 showed the most potent biological activity against HepG2 cells, with an IC 50 value of 0.25 μ m . Western blot analysis demonstrated that compound 47 inhibited the expression of cyclin B1 and p‐Rb and enhanced the expression of p21, p53, Rb, and phospho‐adenosine monophosphate‐activated protein kinase (p‐ AMPK ). Further, cell cycle arrest was observed by flow cytometry ( FCM ). In summary, compound 47 was screened to have potential activity for the treatment of hepatocarcinoma via the induction of cell cycle arrest by a p53/p21‐dependent pathway.