2. Academic Validation
  3. Synthesis and evaluation of aroylthiourea derivatives of 4-β-amino-4'-O-demethyl-4-desoxypodophyllotoxin as novel topoisomerase II inhibitors

Synthesis and evaluation of aroylthiourea derivatives of 4-β-amino-4'-O-demethyl-4-desoxypodophyllotoxin as novel topoisomerase II inhibitors

  • Eur J Med Chem. 2011 Mar;46(3):901-6. doi: 10.1016/j.ejmech.2011.01.001.
Yu Zhao 1,  Cun Wang Ge,  Zhong Hua Wu,  Cheng Niu Wang,  Jing Huai Fang,  Li Zhu
Affiliations

Affiliation

  • 1 Institute of Nautical Medicine, Nantong University, 19 Qixiu Road, Nantong 226001, China.
PMID: 21277655 DOI: 10.1016/j.ejmech.2011.01.001
Abstract

A novel series of aroylthiourea derivatives of 4-β-amino-4'-O-demethyl-4-desoxy- podophyllotoxin were synthesized. Their cytotoxicities against three Cancer cell lines were investigated by MTT assay. The kDNA decatenation assay indicated that compounds 5a, 5f, 5h and 5l inhibited Topoisomerase II-mediated kDNA decatenation. DNA flow cytometric analysis revealed that compound 5a induced cell cycle arrest at G2/M phase in HCT-116 cell line.

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