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Biological evaluation of carbazoyl hydrazine derivatives as potential Pim-1 kinase inhibitors for the treatment of human liver cancer
被引:2
|作者:
Chen, Chong-Hao
[1
,2
]
Xu, Meng-Jia
[1
,3
,4
]
Zheng, Qi
[2
]
Li, Dong-Dong
[3
]
Cheng, Li
[1
]
Sun, Juan
[2
]
Wu, Zi-Miao
[1
]
机构:
[1] Wenzhou Med Univ, Affiliated Cixi Hosp, Ningbo 315300, Peoples R China
[2] Zhejiang Univ Sci & Technol, Sch Biol & Chem Engn, Hangzhou 310023, Peoples R China
[3] Nanjing Forestry Univ, Coll Chem Engn, Nanjing 210037, Peoples R China
[4] Nanjing Agr Univ, Coll Food Sci & Technol, Nanjing 210095, Peoples R China
基金:
中国国家自然科学基金;
关键词:
Carbazole;
Hydrazine;
Molecular docking;
Pim-1;
Antitumor;
POTENCIES;
TARGETS;
D O I:
10.1016/j.molstruc.2023.136742
中图分类号:
O64 [物理化学(理论化学)、化学物理学];
学科分类号:
070304 ;
081704 ;
摘要:
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 Pim1 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.
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