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Structural modification and antitumor activity of the ACLY inhibitor dehydrocurvularin
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Dan-jin WANG1, Qiu-guo GAO1, Shu-qin WANG2, *, Zhang-shuang DENG3, Jian-jia LIANG3, *
Acta Pharmaceutica Sinica | 2025, 60(6) : 1799 - 1806
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Acta Pharmaceutica Sinica | 2025, 60(6): 1799-1806
• Original Articles •
Structural modification and antitumor activity of the ACLY inhibitor dehydrocurvularin
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Dan-jin WANG1, Qiu-guo GAO1, Shu-qin WANG2, *, Zhang-shuang DENG3, Jian-jia LIANG3, *
Affiliations
  • 1Yichang Hec Changjiang Pharmaceutical Co., Ltd., Yidu 443000, China
  • 2College of Medicine, Jingchu University of Technology, Jingmen 448000, China
  • 3Hubei Key Laboratory of Natural Products Research and Development, College of Biological and Pharmaceutical Sciences, China Three Gorges University, Yichang 443002, China
Published: 2025-06-12 doi: 10.16438/j.0513-4870.2024-1286
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A total synthesis of dehydrocurvularin (DCV) demethylated derivatives and structure modification have been completed using a Friedel-Crafts reaction and a highly olefin metathesis reaction. All compounds were identified by NMR, HRMS, etc. Their antitumor activity with high expression of ATP-citrate lyase was evaluated by CCK-8 assay in MDA-MB-231 and HepG2 cells. The structure activity relationship studies were also investigated. Among them, compound 7e showed better antitumor activity than DCV, and could significantly induce apoptosis in MDA-MB-231 cells. These results represent a step toward the development of novel and improved DCV derivatives.

structure modification  /  ATP-citrate lyase  /  antitumour  /  molecular simulation  /  structure activity relationship
王丹津, 郜秋果, 王淑琴, 邓张双, 梁坚家. ACLY抑制剂脱氢弯孢霉菌素的结构改造及抗肿瘤活性研究. 药学学报, 2025 , 60 (6) : 1799 -1806 . DOI: 10.16438/j.0513-4870.2024-1286
Dan-jin WANG, Qiu-guo GAO, Shu-qin WANG, Zhang-shuang DENG, Jian-jia LIANG. Structural modification and antitumor activity of the ACLY inhibitor dehydrocurvularin[J]. Acta Pharmaceutica Sinica, 2025 , 60 (6) : 1799 -1806 . DOI: 10.16438/j.0513-4870.2024-1286
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Year 2025 volume 60 Issue 6
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doi: 10.16438/j.0513-4870.2024-1286
  • Receive Date：2024-12-25
  • Online Date：2026-09-20
  • Published：2025-06-12
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History
  • Received：2024-12-25
  • Revised：2025-03-05
Affiliations
    1Yichang Hec Changjiang Pharmaceutical Co., Ltd., Yidu 443000, China
    2College of Medicine, Jingchu University of Technology, Jingmen 448000, China
    3Hubei Key Laboratory of Natural Products Research and Development, College of Biological and Pharmaceutical Sciences, China Three Gorges University, Yichang 443002, 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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