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Design, synthesis and anti-tumor activity evaluation of quinoline derivatives as histone deacetylase 8 inhibitors
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Yi ZHOU1, Wen-qing SHAO1, Xin-ying YANG2, Xu-ben HOU2, *, Hao FANG2, *
Acta Pharmaceutica Sinica | 2024, 59(4) : 979 - 986
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Acta Pharmaceutica Sinica | 2024, 59(4): 979-986
• Original Articles •
Design, synthesis and anti-tumor activity evaluation of quinoline derivatives as histone deacetylase 8 inhibitors
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Yi ZHOU1, Wen-qing SHAO1, Xin-ying YANG2, Xu-ben HOU2, *, Hao FANG2, *
Affiliations
  • 1. Department of Pharmacy, Shandong Provincial Hospital Affiliated to Shandong First Medical University, Ji'nan 250021, China
  • 2. Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Science, Cheeloo College of Medicine, Shandong University, Ji'nan 250012, China
Published: 2024-04-12 doi: 10.16438/j.0513-4870.2023-0523
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As a member of class I histone deacetylase (HDACs), HDAC8 is an important anticancer drug target. Based on our previously developed pharmacophore model for the HDAC8 inhibitor, we designed and synthesized 13 quinoline acid derivatives as new HDAC8 inhibitors. Among them, the compound SDFZ-E2 and SDFZ-E3 exhibited good HDAC8 inhibitory activities and isoform selectivity. In cell experiments, the target compounds SDFZ-E2 and SDFZ-E3 showed better antiproliferation activities than the known HDAC8 selective inhibitor PCI-34051. In addition, the proposed binding mode of SDFZ-E2 was investigated using molecular docking and molecular dynamics simulation. This work is a new attempt to develop HDAC8 selective inhibitor using quinoline as the scaffold, and the active compounds could serve as lead compounds for further structural optimization.

quinoline derivative  /  histone deacetylase 8 inhibitor  /  anti-tumor activity  /  pharmacophore model
Yi ZHOU, Wen-qing SHAO, Xin-ying YANG, Xu-ben HOU, Hao FANG. Design, synthesis and anti-tumor activity evaluation of quinoline derivatives as histone deacetylase 8 inhibitors[J]. Acta Pharmaceutica Sinica, 2024 , 59 (4) : 979 -986 . DOI: 10.16438/j.0513-4870.2023-0523
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Article Info
doi: 10.16438/j.0513-4870.2023-0523
  • Receive Date：2023-06-28
  • Online Date：2025-11-28
  • Published：2024-04-12
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  • Received：2023-06-28
  • Revised：2023-11-28
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Affiliations
    1. Department of Pharmacy, Shandong Provincial Hospital Affiliated to Shandong First Medical University, Ji'nan 250021, China
    2. Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Science, Cheeloo College of Medicine, Shandong University, Ji'nan 250012, 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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