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Design and synthesis of dehydrocurvularin cinnamy-based ACLY inhibitors for cancer treatment
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Cheng WANG1, Xian-fei CHEN1, Xiang-feng ZHOU1, Xu CHANG2, Zhang-shuang DENG1, 2, *, Jian-jia LIANG1, 2, *
Acta Pharmaceutica Sinica | 2026, 61(7) : 2577 - 2585
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Acta Pharmaceutica Sinica | 2026, 61(7): 2577-2585
• Original Articles •
Design and synthesis of dehydrocurvularin cinnamy-based ACLY inhibitors for cancer treatment
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Cheng WANG1, Xian-fei CHEN1, Xiang-feng ZHOU1, Xu CHANG2, Zhang-shuang DENG1, 2, *, Jian-jia LIANG1, 2, *
Affiliations
  • 1Hubei Key Laboratory of Natural Products Research and Development, College of Biological and Pharmaceutical Sciences, China Three Gorges University, Yichang 443002, China
  • 2Hubei Key Laboratory of Yeast Function, Angel Yeast Co. Ltd., Yichang 443003, China
Published: 2026-07-12 doi: 10.16438/j.0513-4870.2025-1454
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ATP-citrate lyase (ACLY), serving as a critical energy metabolism bridge in tumor cells, is closely implicated in the development of various malignancies. Inhibition or knockout of ACLY has been reported to effectively suppress tumor cell proliferation and induce apoptosis. In this work, we have designed and synthesized 18 dehydrocurvularin cinnamy ACLY inhibitors. Through biological evaluation and molecular dynamics simulations, we systematically explored the structure-activity relationships (SAR) of these derivatives. Compound 4e exhibited potent anti-proliferative activity against MDA-MB-231 and PANC-1 cells with a IC50 value of 0.4 and 1.1 μmol·L-1, providing crucial insights for structural modification and SAR studies of this class of macrolide derivatives.

ATP-citrate lyase  /  structure modification  /  antitumour  /  molecular dynamics simulation  /  structure activity relationship
王程, 陈贤飞, 周向锋, 常煦, 邓张双, 梁坚家. 脱氢弯孢霉素肉桂酰类ACLY抑制剂的设计、合成及抗肿瘤活性研究. 药学学报, 2026 , 61 (7) : 2577 -2585 . DOI: 10.16438/j.0513-4870.2025-1454
Cheng WANG, Xian-fei CHEN, Xiang-feng ZHOU, Xu CHANG, Zhang-shuang DENG, Jian-jia LIANG. Design and synthesis of dehydrocurvularin cinnamy-based ACLY inhibitors for cancer treatment[J]. Acta Pharmaceutica Sinica, 2026 , 61 (7) : 2577 -2585 . DOI: 10.16438/j.0513-4870.2025-1454
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Year 2026 volume 61 Issue 7
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Article Info
doi: 10.16438/j.0513-4870.2025-1454
  • Receive Date：2025-12-04
  • Online Date：2026-09-21
  • Published：2026-07-12
Article Data
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History
  • Received：2025-12-04
  • Revised：2026-01-07
Affiliations
    1Hubei Key Laboratory of Natural Products Research and Development, College of Biological and Pharmaceutical Sciences, China Three Gorges University, Yichang 443002, China
    2Hubei Key Laboratory of Yeast Function, Angel Yeast Co. Ltd., Yichang 443003, 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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