Biological evaluation of carbazoyl hydrazine derivatives as potential Pim-1 kinase inhibitors for the treatment of human liver cancer.

• Our study provides valuable insights into the anticancer activity of novel carbazoyl hydrazine derivatives as Pim-1 inhibitors in liver cancer cells. • Molecular docking studies were performed to evaluate the putative bonding mode of the synthesized compounds (4a-4 s). • Lead compound 4r demonstrates promising potential for further exploration and development in future studies for liver cancer treatment. In this study, we investigated the anticancer activity of novel carbazoyl hydrazine derivatives as inhibitors of Proviral Integration site for Moloney murine leukemia virus kinase 1 (Pim-1) in liver cancer cells in vitro. The obtained compounds were characterized using 1H NMR, 13C NMR, HRMS, and FTIR. Through computer-assisted screening, antitumor activity testing, and Pim-1 inhibitory activity testing, most of the compounds exhibited significant inhibitory activity against liver cancer cell lines. Among them, compound N'-(2-(9H-carbazol-9-yl)acetyl)-4-fluorobenzohydrazide (4r) demonstrated a remarkable anticancer effect by inducing G2/M phase cell cycle arrest and apoptosis. It was identified as a highly efficient lead compound in our screening process. Overall, our study provides valuable insights into the anticancer activity of novel carbazoyl hydrazine derivatives as Pim-1 inhibitors in liver cancer cells. The identified lead compound 4r demonstrates promising potential for further exploration and development in future studies for liver cancer treatment. [Display omitted] [ABSTRACT FROM AUTHOR]