异噁唑烷衍生物对乳腺癌细胞具有选择性抗肿瘤活性

Wijdan Abbas Eneama, Husam Hamza Salman, Mazin N`adhim Mousa
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摘要

乳腺癌是导致女性癌症相关死亡的主要原因之一,因此必须采取有效的治疗干预措施。杂环化合物在美国食品及药物管理局批准的药品中很常见,在药物开发中发挥着关键作用。本研究的重点是异噁唑烷衍生物,这是含氮和含氧杂环的一个亚类,因其在抗肿瘤方面的应用潜力而闻名。研究人员合成了一系列新型异噁唑烷化合物,并使用 MTT 法评估了它们对 MCF-7 和 HdFn 细胞系以及正常细胞的抗癌功效。利用傅立叶变换红外光谱、13C-NMR、1H-NMR 和 E-I 质谱进行了结构阐释。结果显示,化合物(IZ3)的 IC50 值为 32.49 µg/ml,与 HdFn 相比,在 MCF-7 细胞中具有显著的抗肿瘤活性。值得注意的是,化合物(IZ1 和 IZ2)的 IC50 值分别为 64 µg/ml 和 128 µg/ml。这些发现强调了异噁唑烷衍生物作为乳腺癌靶向疗法候选化合物的潜力,值得在临床前模型和临床试验中进一步研究。 亮点: 新型异噁唑烷化合物:合成和评估选择性抗肿瘤活性:在 MCF-7 乳腺癌细胞中显示出有望治疗的候选化合物:用于乳腺癌靶向治疗的异噁唑烷衍生物 关键词:乳腺癌 异噁唑烷衍生物 抗肿瘤活性 杂环化合物 药物开发
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Isoxazolidine Derivatives Exhibit Selective Antitumor Activity Against Breast Cancer Cells
Breast cancer, a leading cause of cancer-related mortality in women, necessitates effective therapeutic interventions. Heterocyclic compounds, prevalent in FDA-approved pharmaceuticals, play a pivotal role in drug development. This study focuses on isoxazolidine derivatives, a subgroup of nitrogen and oxygen-containing heterocycles, known for their potential in antitumor applications. A series of novel isoxazolidine compounds were synthesized and evaluated for their anticancer efficacy using MTT assays against MCF-7 and HdFn cell lines, alongside normal cells. Structural elucidation employed FT-IR, 13C-NMR, 1H-NMR, and E-I mass spectroscopy. Results revealed compound (IZ3) with an IC50 value of 32.49 µg/ml, demonstrating notable antitumor activity in MCF-7 cells compared to HdFn. Notably, compounds (IZ1 and IZ2) exhibited IC50 values of 64 µg/ml and 128 µg/ml, respectively. These findings underscore the potential of isoxazolidine derivatives as promising candidates for targeted breast cancer therapies, warranting further investigation in preclinical models and clinical trials. Highlight: Novel Isoxazolidine Compounds: Synthesized and Evaluated Selective Antitumor Activity: Demonstrated in MCF-7 Breast Cancer Cells Promising Therapeutic Candidates: Isoxazolidine Derivatives for Targeted Breast Cancer Therapy Keyword: Breast cancer, Isoxazolidine Derivatives, Antitumor Activity, Heterocyclic Compounds, Drug Development
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