title: Evaluation of indenoisoquinoline topoisomerase I inhibitors using a hollow fiber assay.
abstract: The indenoisoquinolines are a novel class of non-camptothecin topoisomerase I (Top1) inhibitors whose mechanism of action involves trapping the covalent complex formed between DNA and Top1 during cellular processes. As an ongoing evaluation of the indenoisoquinolines for Top1 inhibition and anticancer activity, indenoisoquinoline analogs have been screened in the National Cancer Institute's hollow fiber assay (HFA). Some of the derivatives demonstrated significant activity at intraperitoneal and subcutaneous fiber placement sites, along with net cancer cell kill in one or more cell lines.
authors.affiliation: Department of Medicinal Chemistry and Molecular Pharmacology and the Purdue Cancer Center, School of Pharmacy and Pharmaceutical Sciences, Purdue University, West Lafayette, IN 47907, USA.
authors.forename: Andrew
authors.initials: A
authors.lastname: Morrell
authors.forename: Muthusamy
authors.initials: M
authors.lastname: Jayaraman
authors.forename: Muthukaman
authors.initials: M
authors.lastname: Nagarajan
authors.forename: Brian M
authors.initials: BM
authors.lastname: Fox
authors.forename: Marintha Rae
authors.initials: MR
authors.lastname: Meckley
authors.forename: Alexandra
authors.initials: A
authors.lastname: Ioanoviciu
authors.forename: Yves
authors.initials: Y
authors.lastname: Pommier
authors.forename: Smitha
authors.initials: S
authors.lastname: Antony
authors.forename: Melinda
authors.initials: M
authors.lastname: Hollingshead
authors.forename: Mark
authors.initials: M
authors.lastname: Cushman
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology*; D001681:Biological Assay / Q000379:methods; D002166:Camptothecin / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D004247:DNA / Q000737:chemistry; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006801:Humans; D007546:Isoquinolines / Q000737:chemistry*; D008956:Models, Chemical; D059004:Topoisomerase I Inhibitors
chemical_list: D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D007546:Isoquinolines; D059004:Topoisomerase I Inhibitors; D004247:DNA; D002166:Camptothecin