Synthesis and Evaluation of Novel Benzofuran Derivatives as Selective SIRT2 Inhibitors
Abstract
:1. Introduction
2. Result and Discussion
2.1. Chemistry
2.2. Sirtuin-Inhibitory Activity Evaluation
3. Experimental Section
3.1. Chemistry
3.2. Synthesis of Compounds 6a–6j
3.3. Synthesis of Compounds 7a–7j
3.4. Biological Evaluation
3.4.1. Expression and Purification of SIRT1−3
3.4.2. SIRT1-3 Assay
4. Conclusions
Supplementary Materials
Acknowledgments
Author Contributions
Conflicts of Interest
References
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Sample Availability: Samples of the compounds 6a–6j and 7a–7j are available from the authors. |
Compd. | R | R1 | IC50 (µM) | ||
---|---|---|---|---|---|
SIRT1 | SIRT2 | SIRT3 | |||
6a | CH3O | CH3O | >100 | 13.52 | >100 |
6b | CH3O | CN | >100 | 15.14 | >100 |
6c | CH3O | Br | >100 | 85.14 | >100 |
6d | CH3O | F | >100 | 95.21 | >100 |
6e | CH3O | CH3OCO | >100 | 15.68 | >100 |
6f | F | CH3O | >100 | 27.89 | >100 |
6g | F | CN | >100 | 32.75 | >100 |
6h | F | Br | >100 | 74.93 | >100 |
6i | F | F | >100 | 88.07 | >100 |
6j | F | CH3OCO | >100 | 19.70 | >100 |
7a | CH3O | CH3O | >100 | 7.66 | >100 |
7b | CH3O | CN | >100 | 8.09 | >100 |
7c | CH3O | Br | >100 | 17.76 | >100 |
7d | CH3O | F | >100 | 43.93 | >100 |
7e | CH3O | CH3OCO | >100 | 3.81 | >100 |
7f | F | CH3O | >100 | 7.92 | >100 |
7g | F | CN | >100 | 8.85 | >100 |
7h | F | Br | >100 | 20.14 | >100 |
7i | F | F | >100 | 51.42 | >100 |
7j | F | CH3OCO | >100 | 6.16 | >100 |
Tenovin6 | - | - | 37.50 | 15.32 | 89.31 |
AGK2 | - | - | >100 | 1.56 | 52.80 |
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Zhou, Y.; Cui, H.; Yu, X.; Peng, T.; Wang, G.; Wen, X.; Sun, Y.; Liu, S.; Zhang, S.; Hu, L.; et al. Synthesis and Evaluation of Novel Benzofuran Derivatives as Selective SIRT2 Inhibitors. Molecules 2017, 22, 1348. https://doi.org/10.3390/molecules22081348
Zhou Y, Cui H, Yu X, Peng T, Wang G, Wen X, Sun Y, Liu S, Zhang S, Hu L, et al. Synthesis and Evaluation of Novel Benzofuran Derivatives as Selective SIRT2 Inhibitors. Molecules. 2017; 22(8):1348. https://doi.org/10.3390/molecules22081348
Chicago/Turabian StyleZhou, Yumei, Huaqing Cui, Xiaoming Yu, Tao Peng, Gang Wang, Xiaoxue Wen, Yunbo Sun, Shuchen Liu, Shouguo Zhang, Liming Hu, and et al. 2017. "Synthesis and Evaluation of Novel Benzofuran Derivatives as Selective SIRT2 Inhibitors" Molecules 22, no. 8: 1348. https://doi.org/10.3390/molecules22081348