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Structurally novel HDAC inhibitors based on the trans-β-arylacryl tetrahydroisoquinoline scaffold: the design, synthesis, and anti-cancer activity
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Xin GAO1, Wei-wei HAN1, Shi-yi TIAN1, Fang FANG1, 2, 3, *, Xiao-dong MA1, 2, 3, Hua-yi CHAI1, Jing-jing HAN1
Acta Pharmaceutica Sinica | 2023, 58(2) : 413 - 422
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Acta Pharmaceutica Sinica | 2023, 58(2): 413-422
• Original Articles •
Structurally novel HDAC inhibitors based on the trans-β-arylacryl tetrahydroisoquinoline scaffold: the design, synthesis, and anti-cancer activity
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Xin GAO1, Wei-wei HAN1, Shi-yi TIAN1, Fang FANG1, 2, 3, *, Xiao-dong MA1, 2, 3, Hua-yi CHAI1, Jing-jing HAN1
Affiliations
  • 1. College of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012, China
  • 2. Department of Medicinal Chemistry, Anhui Academy of Chinese Medicine, Hefei 230012, China
  • 3. Anhui Province Key Laboratory of Research & Development of Chinese Medicine, Hefei 230012, China
Published: 2023-02-12 doi: 10.16438/j.0513-4870.2022-1083
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In this study, a series of 18 histone deacetylases inhibitors (HDACis), derived from our in-house anti-cancer trans-β-arylacryl 1, 2, 3, 4-tetrahydroisoquinoline-based scaffold, were designed, synthesized, and antitumor evaluated. HDAC1 inhibitory activity assay showed that compounds 13d-13f and 13m-13o demonstrated attractive enzymatic activity with IC50 at single-digit nanomolar or subnanomolar level.In addition, 13o exerted superior anti-proliferative activity (A549, IC50 = 0.89 μmol·L-1; HCT116, IC50 = 0.49 μmol·L-1) to that of vorinostat (SAHA).Besides, 13e, with the most potent HDAC1 enzymatic activity (IC50 = 3.8 nmol·L-1), also displayed attractive cellular activity (A549, IC50 = 1.74 μmol·L-1; HCT116, IC50 = 2.43 μmol·L-1). The Western blot analysis illustrated that 13e treatment increased the acetylation of H3 and α-tubulin in a dose-dependent manner in A549 cells. In summary, 13e and 13o deserve further functional investigation.

HDAC inhibitor  /  tetrahydroisoquinoline  /  trans-β-arylacryl  /  anti-cancer
Xin GAO, Wei-wei HAN, Shi-yi TIAN, Fang FANG, Xiao-dong MA, Hua-yi CHAI, Jing-jing HAN. Structurally novel HDAC inhibitors based on the trans-β-arylacryl tetrahydroisoquinoline scaffold: the design, synthesis, and anti-cancer activity[J]. Acta Pharmaceutica Sinica, 2023 , 58 (2) : 413 -422 . DOI: 10.16438/j.0513-4870.2022-1083
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Year 2023 volume 58 Issue 2
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Article Info
doi: 10.16438/j.0513-4870.2022-1083
  • Receive Date：2022-09-29
  • Online Date：2025-11-21
  • Published：2023-02-12
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History
  • Received：2022-09-29
  • Revised：2022-11-03
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Affiliations
    1. College of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012, China
    2. Department of Medicinal Chemistry, Anhui Academy of Chinese Medicine, Hefei 230012, China
    3. Anhui Province Key Laboratory of Research & Development of Chinese Medicine, Hefei 230012, 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
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Genus		 种数
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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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