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Design, synthesis and anticancer activity studies of oleanolic acid derivatives targeting mTOR
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Yan-ling SONG*, Ling LI, Zhong-yan LIU, Jie LI, Peng-bo ZHANG
Acta Pharmaceutica Sinica | 2019, 54(2) : 335 - 342
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Acta Pharmaceutica Sinica | 2019, 54(2): 335-342
Original Articles
Design, synthesis and anticancer activity studies of oleanolic acid derivatives targeting mTOR
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Yan-ling SONG*, Ling LI, Zhong-yan LIU, Jie LI, Peng-bo ZHANG
Affiliations
  • Institute of Pharmaceutical and Biological Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China
Published: 2019-02-12 doi: 10.16438/j.0513-4870.2018-0890
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Ten novel oleanolic acid (OA) derivatives containing urea or thiourea group were designed and synthesized, the chemical structures were confirmed by 1H NMR, 13C NMR and HR-MS. All of these compounds were evaluated for the inhibitory activity against growth of HepG2 and SGC7901 cells. The results showed that compounds I3 and 3 exhibited significant antitumor activities with IC50 of 9.4 and 5.5 μmol·L-1, respectively. Molecular docking studies showed that all these compounds exhibit inhibitory ability against mTOR kinase. Compounds I3 and 3 were further evaluated for the inhibitory activity against mTOR kinase. The results showed that I3 and 3 exhibited strong inhibitory effect on mTOR kinase with IC50 values of 0.83 and 0.26 μmol·L-1.

oleanolic acid derivative  /  synthesis  /  molecular docking  /  anti-tumor activity
Yan-ling SONG, Ling LI, Zhong-yan LIU, Jie LI, Peng-bo ZHANG. Design, synthesis and anticancer activity studies of oleanolic acid derivatives targeting mTOR[J]. Acta Pharmaceutica Sinica, 2019 , 54 (2) : 335 -342 . DOI: 10.16438/j.0513-4870.2018-0890
Year 2019 volume 54 Issue 2
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Article Info
doi: 10.16438/j.0513-4870.2018-0890
  • Receive Date:2018-09-30
  • Online Date:2026-01-26
  • Published:2019-02-12
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  • Received:2018-09-30
  • Revised:2018-10-29
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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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