論文 - 詳細
| RRC ID | 74909 |
|---|---|
| 著者 | Radwan MO, Toma T, Arakaki Y, Kamo M, Inoue N, Koga R, Otsuka M, Tateishi H, Fujita M. |
| タイトル | New insight into the bioactivity of substituted benzimidazole derivatives: Repurposing from anti-HIV activity to cell migration inhibition targeting hnRNP M. |
| ジャーナル | Bioorg Med Chem |
| Abstract |
Drug repurposing is a distinguished approach for drug development that saves a great deal of time and money. Based on our previous successful repurposing of a compound BMMP from anti-HIV-1 therapy to anti-cancer metastatic activity, we adopted the same techniques for repurposing benzimidazole derivatives considering MM-1 as a lead compound. An extensive structure-activity relationship (SAR) study afforded three promising compounds, MM-1d, MM-1h, and MM-1j, which inhibited cell migration in a similar fashion to BMMP. These compounds suppressed CD44 mRNA expression, whereas only MM-1h further suppressed mRNA expression of the epithelial-mesenchymal transition (EMT) marker zeb 1. Using benzimidazole instead of methyl pyrimidine as in BMMP resulted in better affinity for heterogeneous nuclear ribonucleoprotein (hnRNP) M protein and higher anti-cell migration activity. In conclusion, our study identified new agents that surpass the affinity of BMMP for hnRNP M and have anti-EMT activity, which makes them worthy of future attention and optimization. |
| 巻・号 | 86 |
| ページ | 117294 |
| 公開日 | 2023-4-25 |
| DOI | 10.1016/j.bmc.2023.117294 |
| PII | S0968-0896(23)00142-6 |
| PMID | 37141680 |
| MeSH | Cell Line, Tumor Cell Migration Inhibition Drug Repositioning* Heterogeneous-Nuclear Ribonucleoprotein Group M* RNA, Messenger / genetics |
| IF | 3.073 |
| オルトメトリクス指標 |
オルトメトリクス指標項目
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| 各媒体での言及数の合計 | 0 |
| 過去6か月間でのオルトメトリクス指標の変動値 | 0.0 |
| リソース情報 | |
| ヒト・動物細胞 | A549 |