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Bioorg Med Chem Lett ; 30(14): 127239, 2020 07 15.
Article in English | MEDLINE | ID: mdl-32527541

ABSTRACT

Endometrial cancer (EC) is one of the most common and fatal gynecological cancers worldwide, but there is no effective treatment for the EC patients of progesterone resistance. Repurposing of existing drugs is a good strategy to discover new candidate drugs. In this text, perphenazine (PPZ), approved for psychosis therapy, was identified as a potential agent for the treatment of both progesterone sensitive and resistant endometrial cancer for the first time. Specifically, perphenazine exhibited good cell proliferation inhibition in Ishikawa (ISK) and KLE cell lines according to the CCK-8 assay and colony formation assay. It also reduced the cell migration of ISK and KLE cell lines in the light of the transwell migration assay. Annexin-V/PI double staining assay suggested that perphenazine could effectively induce ISK and KLE cell apoptosis. Moreover, results of western blot assay indicated perphenazine obviously inhibited the phosphorylation of Akt. Delightedly, PPZ also could significantly attenuate xenograft tumor growth at both 3 mg/kg and 15 mg/kg in mice without influencing the body weights.


Subject(s)
Antineoplastic Agents/pharmacology , Antipsychotic Agents/pharmacology , Drug Repositioning , Endometrial Neoplasms/drug therapy , Perphenazine/pharmacology , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Antipsychotic Agents/chemical synthesis , Antipsychotic Agents/chemistry , Apoptosis/drug effects , Cell Line, Tumor , Cell Movement/drug effects , Cell Proliferation/drug effects , Dose-Response Relationship, Drug , Drug Screening Assays, Antitumor , Endometrial Neoplasms/pathology , Female , Humans , Molecular Structure , Perphenazine/chemical synthesis , Perphenazine/chemistry , Structure-Activity Relationship
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