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Synthesis and Activity of N'-Substitute-4-{3-(Quinoline-6-yl) Urea} Benzoyl Hydrazide Derivatives
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XIE Yule1, YANG Yijing2, ZHAO Shengxian3, HU Hongyu1, *
Chinese Pharmaceutical Journal | 2024, 59(3) : 227 - 234
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Chinese Pharmaceutical Journal | 2024, 59(3): 227-234
Synthesis and Activity of N'-Substitute-4-{3-(Quinoline-6-yl) Urea} Benzoyl Hydrazide Derivatives
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XIE Yule1, YANG Yijing2, ZHAO Shengxian3, HU Hongyu1, *
Affiliations
  • 1 Xingzhi College, Zhejiang Normal University, Lanxi 321100, China
  • 2 School of Pharmaceutical Sciences, Xiamen University, Xiamen 361102, China
  • 3 College of Science and Technology, Ningbo University, Cixi 315302, China
Published: 2024-02-08 doi: 10.11669/cpj.2024.03.005
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OBJECTIVE To design and synthesize N-substituted methylene-3-(4-(pyridin-3-yl)pyrimidin-2-yl)amino)benzohydrazide derivatives, and evaluate their anticancer activities. OBJECTIVE Using 3-aminobenzoic acid ethyl ester as the starting reagent, a series of target compounds 4a-4p were synthesized in a 4-step reaction, and all of the target compounds were structurally characterized by 1H-NMR, 13C-NMR and HRMS. MTT assay was used to detect the inhibitory effect of synthetic compounds on breast cancer cells. RESULTS It's showed that the target compounds had certain inhibitory activity on the growth of breast cancer cells, among which compound 4e was the best one, showing obvious inhibitory effect on breast cancer cells. The IC50 value of breast cancer cell line MCF-7 was (2.30±0.34)μmol·L-1, and the toxicity of 4e to normal mammary epithelial cells was low(IC50>100 μmol·L-1). Thus, 4e is better than the positive drug cisplatin. In addition, 4e could significantly up-regulate the protein expression level of Nur77 and induce the S-phase arrest of MCF-7. CONCLUSION This series of compounds have good anti-cancer activity and are of interest for further study.

benzoylhydrazine derivatives  /  cell proliferation  /  breast cancer  /  Nur77  /  S-phase arrest
XIE Yule, YANG Yijing, ZHAO Shengxian, HU Hongyu. Synthesis and Activity of N'-Substitute-4-{3-(Quinoline-6-yl) Urea} Benzoyl Hydrazide Derivatives[J]. Chinese Pharmaceutical Journal, 2024 , 59 (3) : 227 -234 . DOI: 10.11669/cpj.2024.03.005
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Year 2024 volume 59 Issue 3
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Article Info
doi: 10.11669/cpj.2024.03.005
  • Receive Date：2023-05-17
  • Online Date：2025-11-13
  • Published：2024-02-08
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  • Received：2023-05-17
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Affiliations
    1 Xingzhi College, Zhejiang Normal University, Lanxi 321100, China
    2 School of Pharmaceutical Sciences, Xiamen University, Xiamen 361102, China
    3 College of Science and Technology, Ningbo University, Cixi 315302, China
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https://castjournals.cast.org.cn/joweb/zgyxzz/EN/10.11669/cpj.2024.03.005
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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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