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Design, synthesis and antitumor activity of isatin derivatives as palmitoyl transferase inhibitors
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Wei YU1, Jin-jiao DONG1, Xin-yue ZHU1, Kan YANG1, Zhen-ming LIU2, Xiao-qiang QIAO1, 3, Ya-li SONG1, *
Acta Pharmaceutica Sinica | 2022, 57(4) : 1073 - 1079
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Acta Pharmaceutica Sinica | 2022, 57(4): 1073-1079
• Original Articles •
Design, synthesis and antitumor activity of isatin derivatives as palmitoyl transferase inhibitors
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Wei YU1, Jin-jiao DONG1, Xin-yue ZHU1, Kan YANG1, Zhen-ming LIU2, Xiao-qiang QIAO1, 3, Ya-li SONG1, *
Affiliations
  • 1. College of Pharmaceutical Sciences, Key Laboratory of Pharmaceutical Quality Control of Hebei Province, Hebei University, Baoding 071002, China
  • 2. State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100191, China
  • 3. Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, Hebei University, Baoding 071002, China
Published: 2022-04-12 doi: 10.16438/j.0513-4870.2021-1389
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Based on the chemical structure of known compound, 12 isatin derivatives palmitoyl transferase inhibitors are designed and synthesized using bioisosterism and molecular docking, while their anti-tumor activities in vitro are determined. The structures of the target compounds are confirmed by 1H NMR, 13C NMR and HR-MS. In vitro anti-tumor assay illustrates that compound 5b exhibits similar anti-tumor activity to the control (IC50 = 8.4 μmol·L-1), with IC50 value of 12.0 μmol·L-1 against MCF-7 in which palmitoyl transferase is highly expressed. Compound 4b shows higher inhibitory activity against HeLa (IC50 = 8.1 μmol·L-1) than cisplatin (IC50 = 40.1 μmol·L-1). The molecular docking demonstrates that all compounds could completely enter the site of 3'-adenosine monophosphate-5'-diphosphate (PAP). Taken together, isatin derivatives represent promising compounds for the discovery of novel anti-tumor agents.

isatin derivative  /  palmitoyl transferase  /  synthesis  /  molecular docking  /  anti-tumor activity
Wei YU, Jin-jiao DONG, Xin-yue ZHU, Kan YANG, Zhen-ming LIU, Xiao-qiang QIAO, Ya-li SONG. Design, synthesis and antitumor activity of isatin derivatives as palmitoyl transferase inhibitors[J]. Acta Pharmaceutica Sinica, 2022 , 57 (4) : 1073 -1079 . DOI: 10.16438/j.0513-4870.2021-1389
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doi: 10.16438/j.0513-4870.2021-1389
  • Receive Date：2021-09-22
  • Online Date：2025-12-22
  • Published：2022-04-12
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History
  • Received：2021-09-22
  • Revised：2021-10-13
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Affiliations
    1. College of Pharmaceutical Sciences, Key Laboratory of Pharmaceutical Quality Control of Hebei Province, Hebei University, Baoding 071002, China
    2. State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100191, China
    3. Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, Hebei University, Baoding 071002, 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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