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Design, synthesis and study of anti-tumor activity of thiazolinone urea derivatives bearing aryloxypyridinone fragments
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Bao-hui QI*, Ying YANG, Guo-wei GONG, Huan HE, Xu-peng YUE, Xin XU, Ya-rong WANG
Acta Pharmaceutica Sinica | 2018, 53(10) : 1696 - 1704
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Acta Pharmaceutica Sinica | 2018, 53(10): 1696-1704
• Medicinal Chemistry •
Design, synthesis and study of anti-tumor activity of thiazolinone urea derivatives bearing aryloxypyridinone fragments
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Bao-hui QI*, Ying YANG, Guo-wei GONG, Huan HE, Xu-peng YUE, Xin XU, Ya-rong WANG
Affiliations
  • Department of Bioengineering, Zhuhai Campus of Zunyi Medical University, Zhuhai 519041, China
Published: 2018-10-12 doi: 10.16438/j.0513-4870.2018-0760
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Taking cabozantinib as leading compound, 13 novel small molecular c-Met inhibitors were designed and synthesized based on the obtained structure-activity relationships (SARs) of c-Met inhibitors. The structures of compounds were confirmed by 1H NMR, 13C NMR and HR-MS. In vitro anti-tumor activity was evaluated by MTT method, and the mechanism was preliminarily disclosed by real-time dynamic living cell imaging and flow cytometry analysis. The results indicated that most of compounds showed good inhibition activity against human non-small-cell carcinoma cell A549 and human colorectal cancer cell HT-29 which was superior to cabozantinb. Compounds showed excellent cytotoxity and anti-proliferative activity against HT-29, and promoted cell apoptosis.

aryloxypyridinone  /  thiazolinone ureas  /  design  /  synthesis  /  anti-tumor activity
Bao-hui QI, Ying YANG, Guo-wei GONG, Huan HE, Xu-peng YUE, Xin XU, Ya-rong WANG. Design, synthesis and study of anti-tumor activity of thiazolinone urea derivatives bearing aryloxypyridinone fragments[J]. Acta Pharmaceutica Sinica, 2018 , 53 (10) : 1696 -1704 . DOI: 10.16438/j.0513-4870.2018-0760
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Year 2018 volume 53 Issue 10
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doi: 10.16438/j.0513-4870.2018-0760
  • Receive Date：2018-08-20
  • Online Date：2026-01-15
  • Published：2018-10-12
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  • Received：2018-08-20
  • Revised：2018-08-31
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    Department of Bioengineering, Zhuhai Campus of Zunyi Medical University, Zhuhai 519041, 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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