title: Synthesis and evaluation of aroylthiourea derivatives of 4-β-amino-4'-O-demethyl-4-desoxypodophyllotoxin as novel topoisomerase II inhibitors.
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.
authors.affiliation: Institute of Nautical Medicine, Nantong University, 19 Qixiu Road, Nantong 226001, China.
authors.forename: Yu
authors.initials: Y
authors.lastname: Zhao
authors.forename: Cun Wang
authors.initials: CW
authors.lastname: Ge
authors.forename: Zhong Hua
authors.initials: ZH
authors.lastname: Wu
authors.forename: Cheng Niu
authors.initials: CN
authors.lastname: Wang
authors.forename: Jing Huai
authors.initials: JH
authors.lastname: Fang
authors.forename: Li
authors.initials: L
authors.lastname: Zhu
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002453:Cell Cycle / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D004250:DNA Topoisomerases, Type II / Q000378:metabolism*; D045325:HCT116 Cells; D056945:Hep G2 Cells; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy; D011034:Podophyllotoxin / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology*; D011035:Podophyllum / Q000737:chemistry; D013890:Thiourea / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D059005:Topoisomerase II Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D059005:Topoisomerase II Inhibitors; D004250:DNA Topoisomerases, Type II; D013890:Thiourea; D011034:Podophyllotoxin