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Evaluation of indenoisoquinoline topoisomerase I inhibitors using a hollow fiber assay.
Bioorg Med Chem Lett. 2006 Aug 15; 16(16):4395-9.BM

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.

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Authors+Show Affiliations

Morrell A
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.
Jayaraman M
No affiliation info available
Nagarajan M
No affiliation info available
Fox BM
No affiliation info available
Meckley MR
No affiliation info available
Ioanoviciu A
No affiliation info available
Pommier Y
No affiliation info available
Antony S
No affiliation info available
Hollingshead M
No affiliation info available
Cushman M
No affiliation info available

MeSH

Antineoplastic AgentsBiological AssayCamptothecinCell Line, TumorDNADrug Screening Assays, AntitumorEnzyme InhibitorsHumansIsoquinolinesModels, ChemicalTopoisomerase I Inhibitors

Pub Type(s)

Journal Article
Research Support, N.I.H., Extramural

Language

eng

PubMed ID

16750365

Citation

Morrell, Andrew, et al. "Evaluation of Indenoisoquinoline Topoisomerase I Inhibitors Using a Hollow Fiber Assay." Bioorganic & Medicinal Chemistry Letters, vol. 16, no. 16, 2006, pp. 4395-9.
Morrell A, Jayaraman M, Nagarajan M, et al. Evaluation of indenoisoquinoline topoisomerase I inhibitors using a hollow fiber assay. Bioorg Med Chem Lett. 2006;16(16):4395-9.
Morrell, A., Jayaraman, M., Nagarajan, M., Fox, B. M., Meckley, M. R., Ioanoviciu, A., Pommier, Y., Antony, S., Hollingshead, M., & Cushman, M. (2006). Evaluation of indenoisoquinoline topoisomerase I inhibitors using a hollow fiber assay. Bioorganic & Medicinal Chemistry Letters, 16(16), 4395-9.
Morrell A, et al. Evaluation of Indenoisoquinoline Topoisomerase I Inhibitors Using a Hollow Fiber Assay. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4395-9. PubMed PMID: 16750365.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Evaluation of indenoisoquinoline topoisomerase I inhibitors using a hollow fiber assay. AU - Morrell,Andrew, AU - Jayaraman,Muthusamy, AU - Nagarajan,Muthukaman, AU - Fox,Brian M, AU - Meckley,Marintha Rae, AU - Ioanoviciu,Alexandra, AU - Pommier,Yves, AU - Antony,Smitha, AU - Hollingshead,Melinda, AU - Cushman,Mark, Y1 - 2006/06/05/ PY - 2006/04/12/received PY - 2006/05/11/revised PY - 2006/05/15/accepted PY - 2006/6/6/pubmed PY - 2006/10/7/medline PY - 2006/6/6/entrez SP - 4395 EP - 9 JF - Bioorganic & medicinal chemistry letters JO - Bioorg Med Chem Lett VL - 16 IS - 16 N2 - 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. SN - 0960-894X UR - https://www.unboundmedicine.com/medline/citation/16750365/Evaluation_of_indenoisoquinoline_topoisomerase_I_inhibitors_using_a_hollow_fiber_assay_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0960-894X(06)00586-5 DB - PRIME DP - Unbound Medicine ER -