Analogs of penfluridol as chemotherapeutic agents with reduced central nervous system activity
Analogs of penfluridol as chemotherapeutic agents with reduced central nervous system activity
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DOI：
10.1016/j.bmcl.2018.10.036
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发表时间：
2018-12-15
影响因子：
2.7
通讯作者：
German, Nadezhda A.
中科院分区：
文献类型：
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作者：
Ashraf-Uz-Zaman, Md;Sajib, Md Sanaullah;German, Nadezhda A.
最近的几份报告强调了使用戊氟利多作为化疗药物的可行性，戊氟利多是一种众所周知的抗精神病药物。体内实验证实了戊氟醇在三阴性乳腺癌模型、肺癌模型中的细胞毒活性，并提出进一步的研究来评估其抗癌活性和治疗胶质母细胞瘤的可行性。然而，戊氟醇的抗癌活性在剂量上明显高于抗精神病药物治疗，因此引起了对接受强化药物治疗的患者中枢神经系统潜在副作用的关注。在这项研究中，我们评估了戊氟醇与一组类似物的潜在中枢神经系统毒性。
Several recent reports have highlighted the feasibility of the use of penfluridol, a well-known antipsychotic agent, as a chemotherapeutic agent. In vivo experiments have confirmed the cytotoxic activity of penfluridol in triple-negative breast cancer model, lung cancer model, and further studies have been proposed to assess its anticancer activity and viability for the treatment of glioblastomas. However, penfluridol anticancer activity was observed at a dosage significantly higher than that administered in antipsychotic therapy, thus raising the concern for the potential onset of CNS side effects in patients undergoing intensive pharmacological treatment. In this study, we evaluate the potential CNS toxicity of penfluridol side by side with a set of analogs.