Identification of Mitotic Blockers by Phenotypic Screening of a Clinical Compound Library

Bulletin of the Korean Chemical Society

Chi Hoon Park²  Sang Un Choi³  You Hwa Son³ 

[1] 350 Republic of Korea;600 Republic of Korea;Bio & Drug Discovery Division Korea Research Institute of Chemical Technology Daejeon 305‐Medicinal Chemistry and Pharmacology Korea University of Science and Technology Daejeon 305‐

关键词: Phenotypic screening;    Mitotic arrest;    Anthelmintic;    Drug repositioning;   

DOI  :  10.1002/bkcs.10999

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

A phenotypic assay was performed using a clinical compound library to identify the new anticancer agents. HeLa cells were treated with the clinical compounds for 20 h, and then screened for cell morphology to check the mitotic arrest. A total of 2320 clinical compounds were tested, of which two anthelmintic compounds, oxibendazole and oxfendazole, were found to induce mitotic arrest in HeLa cells. Additionally, cell‐cycle analysis revealed strong G2/M arrest by these anthelmintics. Moreover, the two compounds, especially oxibendazole, exhibited highly cytotoxic effects on several cancer cell lines. In conclusion, we suggest repositioning of the two anthelmintics, oxibendazole and oxfendazole, if normal cells are not affected by these compounds, to cancer treatment.

【 授权许可】

Unknown