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Synthesis of benzimidazole and benzothiazole derivatives as a sirtuins 2 inhibitor
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Yu-mei ZHOU1, 2, 3, Hua-qing CUI3, Xiao-ming YU3, Shou-guo ZHANG2, Tao PENG2, Gang WANG2, Xiao-xue WEN2, Yun-bo SUN2, Shu-chen LIU2, Lin WANG1, 2, *
Acta Pharmaceutica Sinica | 2017, 52(5) : 773 - 778
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Acta Pharmaceutica Sinica | 2017, 52(5): 773-778
Synthesis of benzimidazole and benzothiazole derivatives as a sirtuins 2 inhibitor
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Yu-mei ZHOU1, 2, 3, Hua-qing CUI3, Xiao-ming YU3, Shou-guo ZHANG2, Tao PENG2, Gang WANG2, Xiao-xue WEN2, Yun-bo SUN2, Shu-chen LIU2, Lin WANG1, 2, *
Affiliations
  • 1. College of Life Science and Bioengineering, Beijing University of Technology, Beijing 100124, China
  • 2. Institute of Radiation Medicine, Academy of Military Medical Sciences, Beijing 100850, China
  • 3. Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
Published: 2017-05-12 doi: 10.16438/j.0513-4870.2017-0180
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A series of novel benzimidazole and benzothiazole derivatives were designed and synthesized as inhibitors of SIRT1-SIRT3. The target compounds were synthesized from potassium O-ethyldithiocarbonate through a three-step route. The structures of the obtained compounds were elucidated by 1H NMR and HR-MS. Of all compounds, six showed potent SIRT2-inhibitory activities with IC50 values ranging from 2.8 to 21.2 μmol·L-1. Among them, compound 10c displayed the most potent SIRT2-inhibitory activities (IC50 = 2.8 μmol·L-1), with more than 35-fold selectivity over SIRT1 and SIRT3 (IC50 > 100 μmol·L-1).

design and synthesis  /  benzimidazole  /  benzothiazole  /  sirtuins inhibitor
Yu-mei ZHOU, Hua-qing CUI, Xiao-ming YU, Shou-guo ZHANG, Tao PENG, Gang WANG, Xiao-xue WEN, Yun-bo SUN, Shu-chen LIU, Lin WANG. Synthesis of benzimidazole and benzothiazole derivatives as a sirtuins 2 inhibitor[J]. Acta Pharmaceutica Sinica, 2017 , 52 (5) : 773 -778 . DOI: 10.16438/j.0513-4870.2017-0180
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Article Info
doi: 10.16438/j.0513-4870.2017-0180
  • Receive Date：2017-02-28
  • Online Date：2026-01-14
  • Published：2017-05-12
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History
  • Received：2017-02-28
  • Revised：2017-03-17
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Affiliations
    1. College of Life Science and Bioengineering, Beijing University of Technology, Beijing 100124, China
    2. Institute of Radiation Medicine, Academy of Military Medical Sciences, Beijing 100850, China
    3. Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
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表12种不同金属材料的力学参数
科
Family		 属数
Number of
genus		 种数
Number of
species		 占总种数比例
Percentage of
total species (%)		 属
Genus		 种数
Number of
species		 占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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