Semi-Synthesis of New 1,2,3-Triazole Derivatives of 9-Bromonoscapine and their Anticancer Activities
| Author | Zahra Hasanpour | en |
| Author | Peyman Salehi | en |
| Author | Morteza Bararjanian | en |
| Author | Mohammad-Ali Esmaeili | en |
| Author | Mostafa Alilou | en |
| Author | Maryam Mohebbi | en |
| Issued Date | 2021-04-30 | en |
| Abstract | Novel 1,2,3-triazole-tethered 9-bromonoscapine derivatives were synthesized by the propargylation of N-nornoscapine followed by Huisgen’s 1,3-dipolar cycloaddition of the terminal alkynes with different azides. Cytotoxicity of the products was studied by MTT assay against the MCF-7 breast cancer cell line. Most of the compounds revealed a better cytotoxicity than N-nornoscapine and 9-bromonornoscapine as the parent compounds. Among the synthesized compounds, those with a hydroxylated aliphatic side chain (5p, 5q, and 5r) showed the highest activities (IC50s: 47.2, 37.9, and 32.3 μg/mL, respectively). Molecular docking studies showed that these compounds also had the highest docking scores and effective interactions with binding sites equal to -8.074, -7.425 and -7.820 kcal/mol, respectively. | en |
| DOI | https://doi.org/10.22037/ijpr.2020.113213.14170 | en |
| Keyword | 9-Bromonoscapine | en |
| Keyword | Triazole | en |
| Keyword | Anti-cancer | en |
| Keyword | Click chemistry | en |
| Keyword | Breast cancer | en |
| Publisher | Brieflands | en |
| Title | Semi-Synthesis of New 1,2,3-Triazole Derivatives of 9-Bromonoscapine and their Anticancer Activities | en |
| Type | Original Article | en |
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