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Synthesis, cytotoxicity, and molecular docking of methylated (–)-epigallocatechin-3-gallate-4β-triazolopodophyllotoxin derivatives as novel antitumor agents
| Content Provider | SAGE Publishing |
|---|---|
| Author | Zi, Cheng-Ting Wang, Ze-Hao Shi, Jing Shi, Bo-Ya Zhang, Ning Wu, Yi-Long Xie, Yin-Rong Zhou, Lu Xiao, Chun Wang, Xuan-Jun Sheng, Jun |
| Copyright Year | 2021 |
| Abstract | A series of novel methylated (–)-epigallocatechin-3-gallate-4β-triazolopodophyllotoxin derivatives is synthesized by utilizing the click reaction. Evaluation of their cytotoxicity against a panel of five human cancer cell lines (HL-60, SMMC-7721, A-549, MCF-7, and SW480) using the MTT assay shows that most of these compounds exhibit weak cytotoxicity. It is observed that compound 12 shows the highest activity against A-549 cells with an IC50 value of 10.27 ± 0.90 μM. Molecular docking results suggested that this compound 12 has a higher binding affinity for epidermal growth factor receptor than for tubulin. Our findings support the utility of compound 12 as a novel compound for the further development of anticancer agents. |
| Related Links | https://journals.sagepub.com/doi/pdf/10.1177/17475198211027328?download=true |
| Starting Page | 876 |
| Ending Page | 882 |
| Page Count | 7 |
| ISSN | 17475198 |
| Issue Number | 9-10 |
| Volume Number | 45 |
| Journal | Journal of Chemical Research (CHL) |
| e-ISSN | 20476507 |
| DOI | 10.1177/17475198211027328 |
| Language | English |
| Publisher | Sage Publications UK |
| Publisher Date | 2021-06-29 |
| Publisher Place | London |
| Access Restriction | Open |
| Rights Holder | © The Author(s) 2021 |
| Subject Keyword | click reaction antitumor activity EGCG podophyllotoxin molecular docking |
| Content Type | Text |
| Resource Type | Article |
| Subject | Chemistry |
