617245-73-5Relevant academic research and scientific papers
Evaluation of Novel N-(piperidine-4-yl)benzamide Derivatives as Potential Cell Cycle Inhibitors in HepG2 Cells
Hou, Jin,Zhao, Wei,Huang, Zhi-Ning,Yang, Shao-Mei,Wang, Li-Juan,Jiang, Yu,Zhou, Zhong-Shi,Zheng, Man-Yi,Jiang, Ji-Li,Li, Shan-Hua,Li, Fu-Nan
, p. 223 - 231 (2015)
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.
DIPHENYLAMINE DERIVATIVES
-
Page/Page column 20, (2010/02/11)
The invention relates to compounds of the formula (I) in which: i and j=1; R1 is in position 3 or 4 on the phenyl ring and represents a cyano group, an alkoxy group substituted by halogen, a thioalkyl group, an alkylcarbonyl group or an alkylsulfonyl group; and R2 represents a carboxyl group, an aikoxycarbonyl group, an alkylcarbonyl group, an unsubstituted amide group or a linear or branched alkyl group substituted by a cyano, hydroxyl, carboxyl, aikoxycarbonyl or unsubstituted amide group; and also the pharmaceutically acceptable derivatives, salts, solvates and stereoisomers thereof, including mixtures thereof in all propor-tions.
NITROSO DERIVATIVES OF DIPHENYLAMINE
-
Page/Page column 27-28, (2010/02/11)
The invention relates to a compound of the formula (I) in which: - R1 represents, independently of each other, a halogen atom; an aliphatic hydrocarbon-based group optionally substituted and/or optionally interrupted by one or more oxygen or sulfur atoms; a nitro group; a cyano group; an amino group; a mono- or dialkylamino group; an alkylcarbonyl group; a carboxyl group; an alkylcarbonylamino group; an alkylsulfonyl group; - R2 represents, independently of each other, a cyano group; a hydroxyl group, an alkylcarbonyl group; a carboxyl group; an alkoxycarbonyl group; an unsubstituted amide group; or a linear or branched alkyl group substituted by a cyano, hydroxyl, carboxyl, alkoxycarbonyl or unsubstituted amide group; - i and j independently being 1 to 5, with the exclusion of the compound for which i and j = 1 and R1 = carboxyl and R2 = alkoxycarbonyl or R1 = CF3 and R2 = carboxyl, and also the pharmaceutically acceptable derivatives, salts, solvates and stereoisomers thereof, including mixtures thereof in all proportions.
