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Analogs of penfluridol as chemotherapeutic agents with reduced central nervous system activity.

ABSTRACT: 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.

SUBMITTER: Ashraf-Uz-Zaman M

PROVIDER: S-EPMC6438620 | biostudies-literature | 2018 Dec

REPOSITORIES: biostudies-literature

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Analogs of penfluridol as chemotherapeutic agents with reduced central nervous system activity.

Ashraf-Uz-Zaman Md M Ashraf-Uz-Zaman Md M Sajib Md Sanaullah MS Cucullo Luca L Mikelis Constantinos M CM German Nadezhda A NA

Bioorganic & medicinal chemistry letters 20181024 23-24

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 ad ...[more]

PMID: 30389290

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