Synthesis and evaluation of aroylthiourea derivatives of 4-β-amino-4'-O-demethyl-4-Desoxypodophyllotoxin (cas 19186-35-7) as novel topoisomerase II inhibitors

Add time:07/31/2019    Source:sciencedirect.com

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.

► A series of aroylthiourea derivatives of 4-β-amino-4′-O-demethyl-4-desoxy- podophyllotoxin as novel topoisomerase II Inhibitors were designed and synthesized. Their cytotoxicities and topoisomerase II inhibitory activity were investigated.

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