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Study on the modification and anti-tumor activity of silybin derivatives for CDK4/6 targeted
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Shi-te GAO1, 2, Zhen-yu KUAI3, Zhi-peng ZHANG1, Yan-qiu MENG1, *
Acta Pharmaceutica Sinica | 2023, 58(3) : 721 - 728
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Acta Pharmaceutica Sinica | 2023, 58(3): 721-728
Study on the modification and anti-tumor activity of silybin derivatives for CDK4/6 targeted
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Shi-te GAO1, 2, Zhen-yu KUAI3, Zhi-peng ZHANG1, Yan-qiu MENG1, *
Affiliations
  • 1. Shenyang University of Chemical Technology, Shenyang 110142, China
  • 2. Shenyang Institute of Science and Technology, Shenyang 110166, China
  • 3. Ma'anshan Vocational and Technical College, Ma'anshan 243031, China
Published: 2023-03-12 doi: 10.16438/j.0513-4870.2022-0972
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By using computer-aided drug design, the activities group model which CDK4/6 inhibitors on the market were introduced to silybin C-7, and a series of silybin derivatives were designed and synthesized, and the structure was confirmed by MS, 13C NMR and 1H NMR. The in vitro antitumor activity evaluation of the target compound was carried out by MTT method, and the in vitro anti-tumor activity was carried out in human hepatocellular carcinoma cells (HepG-2). Experimental results show that all compounds are higher than the activity of the parent silybin, of which compound I1 has a certain inhibitory effect on human HepG-2 cells, which is worth further study.

derivative of silybin  /  CDK4/6 inhibitor  /  structural modification  /  anti-tumor activity
Shi-te GAO, Zhen-yu KUAI, Zhi-peng ZHANG, Yan-qiu MENG. Study on the modification and anti-tumor activity of silybin derivatives for CDK4/6 targeted[J]. Acta Pharmaceutica Sinica, 2023 , 58 (3) : 721 -728 . DOI: 10.16438/j.0513-4870.2022-0972
Year 2023 volume 58 Issue 3
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Article Info
doi: 10.16438/j.0513-4870.2022-0972
  • Receive Date:2022-08-08
  • Online Date:2025-11-21
  • Published:2023-03-12
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History
  • Received:2022-08-08
  • Revised:2022-09-15
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Affiliations
    1. Shenyang University of Chemical Technology, Shenyang 110142, China
    2. Shenyang Institute of Science and Technology, Shenyang 110166, China
    3. Ma'anshan Vocational and Technical College, Ma'anshan 243031, China
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表12种不同金属材料的力学参数

Family
属数
Number of
genus
种数
Number of
species
占总种数比例
Percentage of
total species (%)

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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