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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
5
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pubmed:dateCreated |
2010-3-4
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pubmed:abstractText |
On the basis of the superimposition of the crystal structures of norindenoisoquinoline 5 and topotecan (2) bound in the topoisomerase I-DNA covalent complex, as well as molecular docking and quantum chemical calculations, the substituted norindenoisoquinoline 14a was designed by transporting the 9-dimethylaminomethyl group of topotecan to the 10-position of the norindenoisoquinoline 5. The desired compound 14a was synthesized and found to possess topoisomerase I inhibitory activity that was slightly better than that of the starting compound 5. A focused set of 10-substitued norindenoisoquinoline analogues were then synthesized. The imidazole-substituted compound 14c was highly cytotoxic when evaluated in a series of human leukemia, ovarian, and breast cancer cells.
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pubmed:grant |
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pubmed:commentsCorrections |
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
1520-4804
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pubmed:author |
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pubmed:issnType |
Electronic
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pubmed:day |
11
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pubmed:volume |
53
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1979-89
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pubmed:dateRevised |
2011-7-26
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pubmed:meshHeading |
pubmed-meshheading:20155916-Antineoplastic Agents,
pubmed-meshheading:20155916-Cell Line, Tumor,
pubmed-meshheading:20155916-Cell Proliferation,
pubmed-meshheading:20155916-Drug Design,
pubmed-meshheading:20155916-Enzyme Inhibitors,
pubmed-meshheading:20155916-Humans,
pubmed-meshheading:20155916-Indenes,
pubmed-meshheading:20155916-Isoquinolines,
pubmed-meshheading:20155916-Magnetic Resonance Spectroscopy,
pubmed-meshheading:20155916-Models, Molecular,
pubmed-meshheading:20155916-Spectrometry, Mass, Electrospray Ionization,
pubmed-meshheading:20155916-Structure-Activity Relationship,
pubmed-meshheading:20155916-Thermodynamics,
pubmed-meshheading:20155916-Topoisomerase I Inhibitors
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pubmed:year |
2010
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pubmed:articleTitle |
Structure-based design, synthesis, and biological studies of new anticancer norindenoisoquinoline topoisomerase I inhibitors.
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pubmed:affiliation |
Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, and the Purdue University Center for Cancer Research, Purdue University, West Lafayette, Indiana 47907, USA.
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pubmed:publicationType |
Journal Article,
Research Support, N.I.H., Extramural
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