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Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
A cell-based screen for anticancer activity of 13 pyrazolone derivatives
Xiao-Hong Wang1, Xiao-Kun Wang, Yong-Ju Liang
1State Key Laboratory of Oncology in South China, Sun Yat-sen University Cancer center, Guangzhou, Guangdong 510060, P. R. China.
Background And Objective:
Pyrazolone derivatives were reported to have a potent cytotoxicity against some tumor cells. In the present study, we evaluated the cytotoxic activity of a series of pyrazolone derivatives against four human tumor cell lines including HepG2, OVCAR3, KB, and multidrug resistance (MDR) KBv200 cell lines in vitro and in vivo. Additionally, the structure-activity relationships of these compounds were discussed.
Methods:
To analyze the antiproliferative potential of the synthesized compounds against several human tumor cell lines, the 50% inhibitory concentration (IC50) values were determined by MTT assay. Besides, the KBv200 cell xenograft experimental model was established and the sensitivity to the pyrazolone compounds was compared between drug-sensitive parental KB cells and MDR KBv200 cells.
Results:
Of 13 compounds screened, compound 9 presented remarkable anticancer effects, of which IC50 values were (3.24 ± 0.28), (2.58 ± 0.61), (3.81 ± 0.02), and (3.45 ± 0.03) μg/mL in HepG2, OVCAR3, KB and MDR KBv200 cells, respectively (P > 0.05). Furthermore, compound 9 effectively inhibited tumor growth of KBv200 cell xenografts in vivo, the inhibition ratio was 25.37%, 38.43%, and 47.50% for 1.5 mg/kg, 3 mg/kg, and 6 mg/kg of compound 9 groups, respectively.
Conclusion:
Compound 9 was the most promising antitumor agent in this study.
Insights
Compound 9, a pyrazolone derivative, demonstrated significant anticancer activity against multiple human tumor cell lines and inhibited tumor growth in vivo. This compound shows promise as a potent antitumor agent.
Area of Science:
- Medicinal Chemistry
- Pharmacology
- Oncology
Background:
- Pyrazolone derivatives exhibit known cytotoxicity against various cancer cells.
- This study investigates novel pyrazolone derivatives for their anticancer potential.
Purpose of the Study:
- To evaluate the in vitro and in vivo cytotoxic activity of synthesized pyrazolone derivatives against human tumor cell lines.
- To explore structure-activity relationships of these pyrazolone compounds.
- To assess efficacy against multidrug-resistant (MDR) cancer cells.
Main Methods:
- MTT assay was employed to determine the 50% inhibitory concentration (IC50) values against HepG2, OVCAR3, KB, and MDR KBv200 cell lines.
- A KBv200 cell xenograft model was utilized for in vivo efficacy studies.
- Comparative sensitivity analysis was performed between drug-sensitive KB cells and MDR KBv200 cells.
Main Results:
- Compound 9 exhibited potent antiproliferative activity with low IC50 values across all tested cell lines, including MDR KBv200 cells.
- In vivo studies showed compound 9 effectively inhibited KBv200 cell xenograft growth in a dose-dependent manner.
- Compound 9 demonstrated significant antitumor effects, with inhibition ratios reaching up to 47.50% at the highest dose.
Conclusions:
- Compound 9 is identified as the most effective antitumor agent among the tested pyrazolone derivatives.
- The findings suggest compound 9 holds significant potential for further development as a cancer therapeutic.
