Tacrine-Coumarin Derivatives as Topoisomerase Inhibitors with Antitumor Effects on A549 Human Lung Carcinoma Cancer Cell Lines
Abstract
:1. Introduction
2. Results
2.1. Topoisomerase Relaxation Assay
2.2. Intracellular Localization and Cytotoxicity Assays
2.3. MTT Assay
2.4. Quantification of Cell Number and Viability
2.5. Cell Cycle Distribution
2.6. Clonogenic Assay
3. Discussion
4. Materials and Methods
4.1. Compounds
4.2. Topoisomerase Relaxation Assay
4.3. Cell Culture
4.4. Intracellular Localization and Cytotoxicity Assays
4.5. Clonogenic Assay
4.6. Statistical Analysis
5. Conclusions
Author Contributions
Funding
Data Availability Statement
Acknowledgments
Conflicts of Interest
Sample Availability
References
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Compound | a IC50 (× 10−6 M) | |
---|---|---|
24 h | 48 h | |
1a | n.d. | n.d. |
1b | 83.54 | 74.27 |
1c | 42.36 | 27.04 |
1d | 27.25 | 21.22 |
2a | n.d. | n.d. |
2b | 74.05 | 62.33 |
2c | n.d. | 98.68 |
Compound | Concentration (× 10−6 M) | G1 | S | G2 |
---|---|---|---|---|
Control | 0 | 53.77 ± 1.43 | 33.43 ± 0.71 | 12.81 ± 0.94 |
1a | 25 | 57.03 ± 0.86 | 31.02 ± 0.65 | 11.94 ± 1.37 |
50 | 57.88 ± 1.68 | 30.56 ± 0.72 | 11.56 ± 0.99 | |
1b | 25 | 59.08 ± 1.32 | 29.64 ± 0.22 | 11.29 ± 1.36 |
50 | 71.13 ± 1.59 * | 21.72 ± 1.22 * | 7.15 ± 1.29 * | |
1c | 25 | 79.97 ± 1.25 * | 14.64 ± 1.56 * | 5.39 ± 0.9 * |
50 | 91.86 ± 2.24 * | 6.09 ± 1.98 * | 2.05 ± 0.62* | |
1d | 25 | 86.21 ± 1.67 * | 10.73 ± 0.97 * | 3.06 ± 0.85 * |
50 | 80.85 ± 2.30 * | 12.54 ± 3.46 * | 6.61 ± 1.84 * | |
2a | 25 | 55.54 ± 1.43 | 33.00 ± 1.03 | 11.46 ± 1.41 |
50 | 56.94 ±1.20 | 32.06 ± 0.22 | 11.01 ± 1.07 | |
2b | 25 | 58.18 ± 0.35 | 30.51 ± 1.20 | 11.30 ± 0.86 |
50 | 56.69 ± 2.40 | 32.49 ± 1.56 | 10.83 ± 0.9 | |
2c | 25 | 57.03 ± 2.74 | 31.77 ± 1.73 | 11.20 ± 1.21 |
50 | 57.68 ± 1.24 | 31.80 ± 0.6 | 10.51 ± 1.67 |
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Konkoľová, E.; Hudáčová, M.; Hamuľaková, S.; Jendželovský, R.; Vargová, J.; Ševc, J.; Fedoročko, P.; Kožurková, M. Tacrine-Coumarin Derivatives as Topoisomerase Inhibitors with Antitumor Effects on A549 Human Lung Carcinoma Cancer Cell Lines. Molecules 2021, 26, 1133. https://doi.org/10.3390/molecules26041133
Konkoľová E, Hudáčová M, Hamuľaková S, Jendželovský R, Vargová J, Ševc J, Fedoročko P, Kožurková M. Tacrine-Coumarin Derivatives as Topoisomerase Inhibitors with Antitumor Effects on A549 Human Lung Carcinoma Cancer Cell Lines. Molecules. 2021; 26(4):1133. https://doi.org/10.3390/molecules26041133
Chicago/Turabian StyleKonkoľová, Eva, Monika Hudáčová, Slávka Hamuľaková, Rastislav Jendželovský, Jana Vargová, Juraj Ševc, Peter Fedoročko, and Mária Kožurková. 2021. "Tacrine-Coumarin Derivatives as Topoisomerase Inhibitors with Antitumor Effects on A549 Human Lung Carcinoma Cancer Cell Lines" Molecules 26, no. 4: 1133. https://doi.org/10.3390/molecules26041133