Evaluation of indenoisoquinoline topoisomerase I inhibitors using a hollow fiber assay

Bioorg Med Chem Lett. 2006 Aug 15;16(16):4395-9. doi: 10.1016/j.bmcl.2006.05.048. Epub 2006 Jun 5.

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.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Biological Assay / methods
  • Camptothecin / chemistry
  • Camptothecin / pharmacology
  • Cell Line, Tumor
  • DNA / chemistry
  • Drug Screening Assays, Antitumor / methods
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Isoquinolines / chemistry*
  • Models, Chemical
  • Topoisomerase I Inhibitors*

Substances

  • Antineoplastic Agents
  • Enzyme Inhibitors
  • Isoquinolines
  • Topoisomerase I Inhibitors
  • DNA
  • Camptothecin