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.

journal_name

Bioorg Med Chem Lett

authors

Ashraf-Uz-Zaman M,Sajib MS,Cucullo L,Mikelis CM,German NA

doi

10.1016/j.bmcl.2018.10.036

subject

Has Abstract

pub_date

2018-12-15 00:00:00

pages

3652-3657

issue

23-24

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(18)30838-2

journal_volume

28

pub_type

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