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.

Synthesis, in vitro safety and antioxidant activity of new pyrrole hydrazones

“…In order to check the safety profile of the newly synthesized compounds, we have evaluated their effect on the viability of HepG2 cells through the MTT (tetrazolium dye, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. HepG2 cells have proven to be an appropriate system for the preliminary evaluation of cytotoxicity for several chemical compounds (45,46) including selected N-substituted pyrrolyl hydrazones, as they maintain many of the specialized functions of normal human hepatocytes (47,48).…”

Piperidine nucleus in the field of drug discovery

“…Compound 5 (Fig. 13) was found to have the maximum potency with an IC 50 value 15-fold higher than Sorafenib [27].…”

4-(3-Chloroanilino)benzoic acid

“…In this work, the title compound was successfully prepared by a Buchwald-Hartwig reaction (Fig. 3) (Hou et al, 2015) using 4-chlorobenzoic acid and 3-chloroaniline as starting materials. Crystallization was conducted by slow evaporation in avariety of solvents in a clean fume hood.…”