HY-2, a novel DNA topoisomerase II inhibitor, induces G2/M cell cycle arrest in HCT-116 cells.

Zhonghua Wu, Yu Zhao, Yuting Zhang, Li Zhu

Index: J. Chemother. 26(6) , 342-7, (2014)

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Abstract

4beta-(Benzoylthioureido)-4'-demethyl-4-desoxypodophyllotoxin (HY-2), a synthetic aroylthiourea analog of podophyllotoxin, was identified as a novel DNA topoisomerase II inhibitor. It exhibited significant antiproliferative effect on seven cancer cell lines and induced HCT-116 cells apoptosis. DNA flow cytometric analysis revealed that HY-2 induced cell cycle arrest at G2/M phase. Western blot analysis indicated that phosphorylation of cdc2 protein was decreased after HY-2 treatment, which might be the main cause for G2/M phase arrest.