Abstract |
Twenty-six novel isosteviol derivatives coupled with two types of nitric oxide (NO) donors ( furoxans and NONOates) were synthesized and screened for cytotoxic activities against four human cancer cell lines with sunitinib as the positive control. The results showed that seven furoxan-based derivatives (8a, 8b, 8c, 8d, 8e, 9e, and 9f) exhibited desirable cytotoxic activities, while NONOate-based derivatives displayed poor potency because of unstability. Compared with sunitinib, compounds 8a and 8e were more active on all tested cell lines, especially in HCT116 (8a, IC50 = 0.48 ± 0.02 μm; 8e, IC50 = 0.94 ± 0.01 μm); compounds 8b and 8d were more potent on HCT116 (IC50 = 3.39 ± 0.06 and 3.29 ± 0.03 μm), HepG2 (IC50 = 1.05 ± 0.03 and 5.37 ± 0.08 μm), and SW620 (IC50 = 1.33 ± 0.02 and 4.11 ± 0.05 μm) cell lines, and 8c exhibited higher activities on HepG2 cells with an IC50 = 4.76 ± 0.14 μm. NO-releasing experiment of compounds 8a-e, 17a, 18a, 19a, and 21a reminded us that NO-releasing amount of this series of isosteviol derivatives positively correlates with their cytotoxic activities.
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Authors | Yan Liu, Tingting Wang, Yong Ling, Na Bao, Wei Shi, Li Chen, Jianbo Sun |
Journal | Chemical biology & drug design
(Chem Biol Drug Des)
Vol. 90
Issue 3
Pg. 473-477
(Sep 2017)
ISSN: 1747-0285 [Electronic] England |
PMID | 28122177
(Publication Type: Letter)
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Copyright | © 2017 John Wiley & Sons A/S. |
Chemical References |
- Antineoplastic Agents
- Diterpenes, Kaurane
- Nitric Oxide Donors
- isosteviol
- Nitric Oxide
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Topics |
- Antineoplastic Agents
(chemical synthesis, chemistry, pharmacology, toxicity)
- Cell Line, Tumor
- Cell Survival
(drug effects)
- Diterpenes, Kaurane
(chemical synthesis, chemistry, pharmacology, toxicity)
- Drug Design
- Drug Screening Assays, Antitumor
- HCT116 Cells
- Hep G2 Cells
- Humans
- Nitric Oxide
(metabolism)
- Nitric Oxide Donors
(chemical synthesis, chemistry, pharmacology, toxicity)
- Structure-Activity Relationship
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