title: Evaluation of Novel N-(piperidine-4-yl)benzamide Derivatives as Potential Cell Cycle Inhibitors in HepG2 Cells.
abstract: 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 IC50 value of 0.25 μm. 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.
authors.affiliation: School of Pharmaceutical Sciences, Xiamen University, Xiang'an South Road, Xiamen, 361102, China.
authors.forename: Jin
authors.initials: J
authors.lastname: Hou
authors.affiliation: School of Pharmaceutical Sciences, Xiamen University, Xiang'an South Road, Xiamen, 361102, China.
authors.forename: Wei
authors.initials: W
authors.lastname: Zhao
authors.affiliation: School of Pharmaceutical Sciences, Xiamen University, Xiang'an South Road, Xiamen, 361102, China.
authors.forename: Zhi-Ning
authors.initials: ZN
authors.lastname: Huang
authors.affiliation: School of Pharmaceutical Sciences, Xiamen University, Xiang'an South Road, Xiamen, 361102, China.
authors.forename: Shao-Mei
authors.initials: SM
authors.lastname: Yang
authors.affiliation: School of Pharmaceutical Sciences, Xiamen University, Xiang'an South Road, Xiamen, 361102, China.
authors.forename: Li-Juan
authors.initials: LJ
authors.lastname: Wang
authors.affiliation: Department of Outpatient, Air Force of Chengdu Military Command, 87 New South Road, Chengdu, 610041, China.
authors.forename: Yu
authors.initials: Y
authors.lastname: Jiang
authors.affiliation: Department of Basic Medical Sciences of Medical College, Xiamen University, Xiang'an South Road, Xiamen, 361102, China.
authors.forename: Zhong-Shi
authors.initials: ZS
authors.lastname: Zhou
authors.affiliation: School of Pharmaceutical Sciences, Xiamen University, Xiang'an South Road, Xiamen, 361102, China.
authors.forename: Man-Yi
authors.initials: MY
authors.lastname: Zheng
authors.affiliation: School of Pharmaceutical Sciences, Xiamen University, Xiang'an South Road, Xiamen, 361102, China.
authors.forename: Ji-Li
authors.initials: JL
authors.lastname: Jiang
authors.affiliation: Department of Basic Medical Sciences of Medical College, Xiamen University, Xiang'an South Road, Xiamen, 361102, China.
authors.forename: Shan-Hua
authors.initials: SH
authors.lastname: Li
authors.affiliation: School of Pharmaceutical Sciences, Xiamen University, Xiang'an South Road, Xiamen, 361102, China.
authors.forename: Fu-Nan
authors.initials: FN
authors.lastname: Li
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D001549:Benzamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006528:Carcinoma, Hepatocellular / Q000188:drug therapy* / Q000473:pathology; D059447:Cell Cycle Checkpoints / Q000187:drug effects; D050759:Cyclin-Dependent Kinase Inhibitor p21 / Q000378:metabolism; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D056945:Hep G2 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D008113:Liver Neoplasms / Q000188:drug therapy* / Q000473:pathology; D010880:Piperidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D016159:Tumor Suppressor Protein p53 / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D001549:Benzamides; D050759:Cyclin-Dependent Kinase Inhibitor p21; D010880:Piperidines; C495901:TP53 protein, human; D016159:Tumor Suppressor Protein p53
keywords: HepG2; N-(piperidine-4-yl) benzamide derivatives; cell cycle; p53/p21-dependent pathway