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Evaluation of indenoisoquinoline topoisomerase I inhibitors using a hollow fiber assay

  1. Author:
    Morrell, A.
    Jayaraman, M.
    Nagarajan, M.
    Fox, B. M.
    Meckley, M. R.
    Ioanoviciu, A.
    Pommier, Y.
    Antony, S.
    Hollineshead, M.
    Cushman, M.
  2. Author Address

    Purdue Univ, Sch Pharm & Pharmaceut Sci, Dept Med Chem & Mol Pharmacol, W Lafayette, IN 47907 USA. Purdue Univ, Sch Pharm & Pharmaceut Sci, Purdue Canc Ctr, W Lafayette, IN 47907 USA. NCI, Ctr Canc Res, Mol Pharmacol Lab, Bethesda, MD 20892 USA. NCI, Biol Testing Branch, Dev Therapeut Program, Div Canc Treatment & Diag,NIH,Fairview Ctr, Frederick, MD 21701 USA.;Cushman, M, Purdue Univ, Sch Pharm & Pharmaceut Sci, Dept Med Chem & Mol Pharmacol, W Lafayette, IN 47907 USA.;cushman@pharmacy.purdue.edu
    1. Year: 2006
    2. Date: Aug
  1. Journal: Bioorganic & Medicinal Chemistry Letters
    1. 16
    2. 16
    3. Pages: 4395-4399
  2. Type of Article: Article
  3. ISSN: 0960-894X
  1. 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 Top I during cellular processes. As an ongoing evaluation of the indenoisoquitiolines 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. (c) 2006 Elsevier Ltd. All rights reserved.

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External Sources

  1. DOI: 10.1016/j.bmcl.2006.05.048
  2. WOS: 000239349000047

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