Design, Synthesis, and Biological Evaluation of Axitinib Derivatives
Abstract
:1. Introduction
2. Results and Discussion
2.1. Chemistry
2.2. Biological Evaluation
2.2.1. VEGFR-2 Kinase Assay
2.2.2. Molecular Docking Study
2.2.3. HUVEC Cell Anti-Proliferation Assay
3. Materials and Methods
3.1. Chemistry
General Procedure 1
3.2. VEGFR2 Kinase Assay
3.3. Molecular Docking Study
3.4. HUVEC Cell Proliferation Assay
4. Conclusions
Acknowledgments
Author Contributions
Conflicts of Interest
References
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Sample Availability: Samples of the compounds are not available from the authors. |
Compound | IC50 (nM) ± SD (n = 3) |
---|---|
Axitinib | 7.3 ± 1.07 |
TM2 | 3000 ± 1.11 |
TM3 | 195 ± 1.11 |
TM4 | 135 ± 1.25 |
TM6 | 2290 ± 1.17 |
TM7 | 123 ± 1.08 |
TM8 | 158 ± 1.14 |
TM9 | 201 ± 1.26 |
TM10 | 44 ± 1.15 |
TM11 | 330 ± 1.14 |
Compound | Relative Cell Viability (%) ± SD (n = 3) | |
---|---|---|
1 µM | 10 µM | |
Axitinib | 79.97 ± 6.64 | 53.22 ± 9.11 |
TM2 | 106.56 ± 1.29 | 94.40 ± 5.01 |
TM3 | 125.46 ± 8.92 | 84.14 ± 6.83 |
TM4 | 94.12 ± 1.89 | 82.76 ± 5.32 |
TM6 | 96.95 ± 10.44 | 19.33 ± 3.82 |
TM7 | 84.36 ± 4.35 | 39.13 ± 2.49 |
TM8 | 92.34 ± 9.05 | 61.26 ± 10.94 |
TM9 | 68.54 ± 0.29 | 32.20 ± 1.99 |
TM10 | 99.29 ± 0.78 | 66.22 ± 4.43 |
TM11 | 67.03 ± 0.19 | 30.97 ± 0.61 |
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Wei, N.; Liang, J.; Peng, S.; Sun, Q.; Dai, Q.; Dong, M. Design, Synthesis, and Biological Evaluation of Axitinib Derivatives. Molecules 2018, 23, 747. https://doi.org/10.3390/molecules23040747
Wei N, Liang J, Peng S, Sun Q, Dai Q, Dong M. Design, Synthesis, and Biological Evaluation of Axitinib Derivatives. Molecules. 2018; 23(4):747. https://doi.org/10.3390/molecules23040747
Chicago/Turabian StyleWei, Na, Jianqing Liang, Shengming Peng, Qiang Sun, Qiuyun Dai, and Mingxin Dong. 2018. "Design, Synthesis, and Biological Evaluation of Axitinib Derivatives" Molecules 23, no. 4: 747. https://doi.org/10.3390/molecules23040747