Ginkgolide B derivative synthesis and their effects on the viability of SKOV3 cells

The natural product Ginkgolide B was used as a raw material and modified by esterification on C10-OH or C1-OH to obtain 11 derivatives ( 1 – 11 ), which were structurally characterized with nuclear magnetic resonance spectroscopy. An MTT assay-based in vitro tumor proliferation inhibitory activity t...

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Veröffentlicht in:Medicinal chemistry research 2021-06, Vol.30 (6), p.1265-1272
Hauptverfasser: Feng, ZiLi, Zhu, ZhiBin, Chen, Wang, Xu, JiaYuan, Bai, Yu, Hu, DaiHua, Zhao, ZhengDong
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Sprache:eng
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Zusammenfassung:The natural product Ginkgolide B was used as a raw material and modified by esterification on C10-OH or C1-OH to obtain 11 derivatives ( 1 – 11 ), which were structurally characterized with nuclear magnetic resonance spectroscopy. An MTT assay-based in vitro tumor proliferation inhibitory activity test showed that compounds 2 , 3 , 6 , 7 , 10 , and 11 exhibited strong inhibitory activity against the human ovarian cancer cells SKOV3, with IC 50 values of 16.05 µmol/L, 15.65 µmol/L, 32.00 µmol/L, 63.30 µmol/L, 23.20 µmol/L, and 31.10 µmol/L, respectively. Annexin V/PI double staining assay showed that compound 2 induced apoptosis in SKOV3 cells to a slightly greater extent than GB and compounds 5 and 9 , with an apoptosis rate of 31.68%.
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-021-02732-7