A leading cause of death worldwide, breast cancer is the second most prevalent cancer in women. Triple-negative breast cancer is an aggressive subtype that lacks targeted therapies and requires novel therapeutic approaches in clinical practice to improve the overall survival. Theranostic agents that integrate diagnostic and therapeutic capabilities in a single entity are promising strategies for personalized cancer management. Hybrid compounds combining biologically relevant moieties with different modes of action can enhance cytotoxicity and improve pharmacological properties. We focus on a hybrid containing coumarin, triazole, and [10]-gingerol, a compound with known antimetastatic potential in TNBC. The LSPN281 hybrid exhibited superior cytotoxic activity in a TNBC cell line in vitro compared to the individual coumarin and [10]-gingerol controls. Additionally, the hybrid shows enhanced cellular uptake and mitochondrial localization, suggesting its potential as a theranostic agent for TNBC.
Enhanced Cytotoxicity of [10]-Gingerol-Coumarin-Triazole Hybrid as a Theranostic Agent for Triple Negative Breast Cancer.
[10]-姜酚-香豆素-三唑杂合物作为三阴性乳腺癌诊疗剂的增强细胞毒性
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作者:Zutião Arthur Deponte, Pachane Bianca Cruz, Nunes Paulo Sérgio Gonçalves, Vidal Herika Danielle Almeida, Selistre-de-Araujo Heloisa Sobreiro, Corrêa Arlene Gonçalves, Cominetti Marcia Regina, Fuzer Angelina Maria
| 期刊: | ACS Medicinal Chemistry Letters | 影响因子: | 4.000 |
| 时间: | 2025 | 起止号: | 2025 Feb 10; 16(3):436-443 |
| doi: | 10.1021/acsmedchemlett.4c00596 | 研究方向: | 细胞生物学 |
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