| Autor: |
Yingying Tian, Ailin Yang, Huiming Huang, Jinxin Xie, Longyan Wang, Dongxiao Liu, Xuejiao Wei, Peng Tan, Pengfei Tu, Dongjun Fu, Zhongdong Hu |
| Jazyk: |
angličtina |
| Rok vydání: |
2024 |
| Předmět: |
|
| Zdroj: |
Arabian Journal of Chemistry, Vol 17, Iss 2, Pp 105550- (2024) |
| Druh dokumentu: |
article |
| ISSN: |
1878-5352 |
| DOI: |
10.1016/j.arabjc.2023.105550 |
| Popis: |
Hepatocellular carcinoma (HCC) is a major global cause of carcinoma-related fatality. The inhibition of tubulin polymerization holds significant potential in the development of cancer drugs. In our study, we synthesized a novel pyrrolidine-2,5-dione derivative (compound 8) that exhibited potent anti-HCC activity (IC50 value of 2.082 μM) against human HCC HepG2 cells. Moreover, compound 8 significantly suppressed the HepG2 cell multiplication, and triggered G2/M phase arrest of HepG2 cells and their apoptosis. Further mechanistic investigations revealed that compound 8 suppressed tubulin polymerization by directly binding to the colchicine binding site of β-tubulin. Additionally, compound 8 significantly inhibited tumor growth with low toxicity in nude HepG2 tumor-bearing mice, achieving an approximate inhibition rate of 45.73 %. Therefore, compound 8 represents a promising pharmaceutical candidate for HCC management. |
| Databáze: |
Directory of Open Access Journals |
| Externí odkaz: |
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