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Design, synthesis and anti-tumor activity studies of oleanolic acid derivatives using VEGFR as target
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Yan-ling SONG*, Zhong-yan LIU, Ling LI, Jie LI, Peng-bo ZHANG
Acta Pharmaceutica Sinica | 2018, 53(11) : 1852 - 1861
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Acta Pharmaceutica Sinica | 2018, 53(11): 1852-1861
Medicinal Chemistry
Design, synthesis and anti-tumor activity studies of oleanolic acid derivatives using VEGFR as target
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Yan-ling SONG*, Zhong-yan LIU, Ling LI, Jie LI, Peng-bo ZHANG
Affiliations
  • Institute of Pharmaceutical and Biological Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China
Published: 2018-11-12 doi: 10.16438/j.0513-4870.2018-0731
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In this study, twenty containing ethylenediamine groups derivatives of oleanolic acid (OA) were synthesized, their structures were determined by 1H NMR, 13C NMR and HR-MS. The anti-tumor activities in HepG2 and SGC7901 cells were evaluated by MTT assay. The results showed that all compounds exhibited anti-tumor activity, compounds 6, 8 and 9 exhibited significant anti-tumor activities with IC50 values of 16.7, 9.8 and 6.3 μmol·L-1, respectively. Molecular docking studies showed that compounds 6-9 produce higher combining ability with VEGFR. Compound 6-9 were further evaluated for the inhibitory activity against VEGFR-2, the result showed 9 had a strong inhibitory effect on VEGFR with IC50 values of 0.56 μmol·L-1.

oleanolic acid derivative  /  synthesis  /  molecular docking  /  anti-tumor activity
Yan-ling SONG, Zhong-yan LIU, Ling LI, Jie LI, Peng-bo ZHANG. Design, synthesis and anti-tumor activity studies of oleanolic acid derivatives using VEGFR as target[J]. Acta Pharmaceutica Sinica, 2018 , 53 (11) : 1852 -1861 . DOI: 10.16438/j.0513-4870.2018-0731
Year 2018 volume 53 Issue 11
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doi: 10.16438/j.0513-4870.2018-0731
  • Receive Date:2018-08-13
  • Online Date:2026-01-15
  • Published:2018-11-12
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  • Received:2018-08-13
  • Revised:2018-09-13
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    Institute of Pharmaceutical and Biological Engineering, Shenyang University of Chemical Technology, Shenyang 110142, 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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