title: Synthesis, cytotoxicity and topoisomerase II inhibitory activity of lomefloxacin derivatives.
abstract: A novel series of amide derivatives of lomefloxacin were synthesized and evaluated for their topoisomerase I and II inhibitory activity as well as cytotoxicity against a panel of five human cancer cell lines. Of the compounds prepared compounds 9d and 9g exhibited strong inhibition against topoisomerase II at 100μM. In addition, docking studies were performed to predict the inhibition mode.
authors.affiliation: Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China.
authors.forename: You
authors.initials: Y
authors.lastname: Zhou
authors.forename: Xiaoli
authors.initials: X
authors.lastname: Xu
authors.forename: Yuan
authors.initials: Y
authors.lastname: Sun
authors.forename: Huaping
authors.initials: H
authors.lastname: Wang
authors.forename: Haopeng
authors.initials: H
authors.lastname: Sun
authors.forename: Qidong
authors.initials: Q
authors.lastname: You
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004250:DNA Topoisomerases, Type II / Q000378:metabolism*; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D024841:Fluoroquinolones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045325:HCT116 Cells; D006801:Humans; D007624:KB Cells; D008958:Models, Molecular; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D059005:Topoisomerase II Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D024841:Fluoroquinolones; D059005:Topoisomerase II Inhibitors; D004250:DNA Topoisomerases, Type II; C053091:lomefloxacin