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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
13
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pubmed:dateCreated |
2007-6-18
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pubmed:abstractText |
An intramolecular radical cyclization reaction of 4-bromo-3-arylisoquinolines 11a-c allowed the efficient synthesis of 11-methylindenoisoquinolines 2a-c. 5-(2-Aminoethylamino)indeno[1,2-c]isoquinolin-11-one 4 was also prepared in the convenient manner. The synthesized compounds were tested in vitro for cytotoxicity and DNA-topoisomerase 1 (top 1) inhibitory activity. The dramatic enhancement of top 1 inhibitory activity of 4 was explained by a docking study using the FlexX program.
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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 |
Jul
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pubmed:issn |
0960-894X
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
1
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pubmed:volume |
17
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3531-4
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:17498951-Antineoplastic Agents,
pubmed-meshheading:17498951-Cell Line, Tumor,
pubmed-meshheading:17498951-Chemistry, Pharmaceutical,
pubmed-meshheading:17498951-DNA,
pubmed-meshheading:17498951-DNA Topoisomerases, Type I,
pubmed-meshheading:17498951-Drug Design,
pubmed-meshheading:17498951-Drug Screening Assays, Antitumor,
pubmed-meshheading:17498951-Enzyme Inhibitors,
pubmed-meshheading:17498951-Humans,
pubmed-meshheading:17498951-Inhibitory Concentration 50,
pubmed-meshheading:17498951-Isoquinolines,
pubmed-meshheading:17498951-Models, Chemical,
pubmed-meshheading:17498951-Models, Molecular,
pubmed-meshheading:17498951-Topoisomerase Inhibitors,
pubmed-meshheading:17498951-X-Rays
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pubmed:year |
2007
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pubmed:articleTitle |
Design, docking, and synthesis of novel indeno[1,2-c]isoquinolines for the development of antitumor agents as topoisomerase I inhibitors.
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pubmed:affiliation |
College of Pharmacy and Research Institute of Drug Development, Chonnam National University, Kwangju 500-757, Republic of Korea. wjcho@jnu.ac.kr <wjcho@jnu.ac.kr>
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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