Synthesis and Evaluation of Novel Benzofuran Derivatives as Selective SIRT2 Inhibitors
A series of benzofuran derivatives were designed and synthesized, and their inhibitory activites were measured against the SIRT1–3. The enzymatic assay showed that all the compounds showed certain anti-SIRT2 activity and selective over SIRT1 and SIRT3 with IC50 (half maximal inhibitory concentration...
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MDPI AG
2017-08-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/22/8/1348 |
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doaj-d1b4be05482741da8ddc79a579503c5b2020-11-24T21:34:42ZengMDPI AGMolecules1420-30492017-08-01228134810.3390/molecules22081348molecules22081348Synthesis and Evaluation of Novel Benzofuran Derivatives as Selective SIRT2 InhibitorsYumei Zhou0Huaqing Cui1Xiaoming Yu2Tao Peng3Gang Wang4Xiaoxue Wen5Yunbo Sun6Shuchen Liu7Shouguo Zhang8Liming Hu9Lin Wang10College of Life Science and Bioengineering, Beijing University of Technology, Beijing 100124, ChinaInstitute of MateriaMedica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, ChinaInstitute of MateriaMedica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, ChinaInstitute of Radiation Medicine, Academy of Military Medical Sciences, Beijing 100850, ChinaInstitute of Radiation Medicine, Academy of Military Medical Sciences, Beijing 100850, ChinaInstitute of Radiation Medicine, Academy of Military Medical Sciences, Beijing 100850, ChinaInstitute of Radiation Medicine, Academy of Military Medical Sciences, Beijing 100850, ChinaInstitute of Radiation Medicine, Academy of Military Medical Sciences, Beijing 100850, ChinaInstitute of Radiation Medicine, Academy of Military Medical Sciences, Beijing 100850, ChinaCollege of Life Science and Bioengineering, Beijing University of Technology, Beijing 100124, ChinaCollege of Life Science and Bioengineering, Beijing University of Technology, Beijing 100124, ChinaA series of benzofuran derivatives were designed and synthesized, and their inhibitory activites were measured against the SIRT1–3. The enzymatic assay showed that all the compounds showed certain anti-SIRT2 activity and selective over SIRT1 and SIRT3 with IC50 (half maximal inhibitory concentration) values at the micromolar level. The preliminary structure–activity relationships were analyzed and the binding features of compound 7e (IC50 3.81 µM) was predicted using the CDOCKER program. The results of this research could provide informative guidance for further optimizing benzofuran derivatives as potent SIRT2 inhibitors.https://www.mdpi.com/1420-3049/22/8/1348benzofuransulfoxidesulfoneselective SIRT2 inhibitor |
| collection |
DOAJ |
| language |
English |
| format |
Article |
| sources |
DOAJ |
| author |
Yumei Zhou Huaqing Cui Xiaoming Yu Tao Peng Gang Wang Xiaoxue Wen Yunbo Sun Shuchen Liu Shouguo Zhang Liming Hu Lin Wang |
| spellingShingle |
Yumei Zhou Huaqing Cui Xiaoming Yu Tao Peng Gang Wang Xiaoxue Wen Yunbo Sun Shuchen Liu Shouguo Zhang Liming Hu Lin Wang Synthesis and Evaluation of Novel Benzofuran Derivatives as Selective SIRT2 Inhibitors Molecules benzofuran sulfoxide sulfone selective SIRT2 inhibitor |
| author_facet |
Yumei Zhou Huaqing Cui Xiaoming Yu Tao Peng Gang Wang Xiaoxue Wen Yunbo Sun Shuchen Liu Shouguo Zhang Liming Hu Lin Wang |
| author_sort |
Yumei Zhou |
| title |
Synthesis and Evaluation of Novel Benzofuran Derivatives as Selective SIRT2 Inhibitors |
| title_short |
Synthesis and Evaluation of Novel Benzofuran Derivatives as Selective SIRT2 Inhibitors |
| title_full |
Synthesis and Evaluation of Novel Benzofuran Derivatives as Selective SIRT2 Inhibitors |
| title_fullStr |
Synthesis and Evaluation of Novel Benzofuran Derivatives as Selective SIRT2 Inhibitors |
| title_full_unstemmed |
Synthesis and Evaluation of Novel Benzofuran Derivatives as Selective SIRT2 Inhibitors |
| title_sort |
synthesis and evaluation of novel benzofuran derivatives as selective sirt2 inhibitors |
| publisher |
MDPI AG |
| series |
Molecules |
| issn |
1420-3049 |
| publishDate |
2017-08-01 |
| description |
A series of benzofuran derivatives were designed and synthesized, and their inhibitory activites were measured against the SIRT1–3. The enzymatic assay showed that all the compounds showed certain anti-SIRT2 activity and selective over SIRT1 and SIRT3 with IC50 (half maximal inhibitory concentration) values at the micromolar level. The preliminary structure–activity relationships were analyzed and the binding features of compound 7e (IC50 3.81 µM) was predicted using the CDOCKER program. The results of this research could provide informative guidance for further optimizing benzofuran derivatives as potent SIRT2 inhibitors. |
| topic |
benzofuran sulfoxide sulfone selective SIRT2 inhibitor |
| url |
https://www.mdpi.com/1420-3049/22/8/1348 |
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