Source:http://linkedlifedata.com/resource/pubmed/id/20236733
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
6
|
| pubmed:dateCreated |
2010-4-20
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| pubmed:abstractText |
Novel derivatives of 5-(substituted)benzylidene-3-(4-substituted)phenylsulfonylimidazolidine-2,4-diones (3a-r), 1-(4-substituted)phenylsulfonyl-3-(4-substituted)phenylpyrimidine-2,4,6-(1H,3H,5H)-triones (6a-l), and 3-(4-substituted)phenyl-1-(4-substituted)phenylsulfonylquinazoline-2,4(1H,3H)- diones (8a-l) have been synthesized and tested for their antitumor activity against 60 tumor cell lines taken from 9 different organs. The tested compounds have showed good inhibitory effect at the ovarian cancer (IGROV1) cell line. A significant inhibition for (RXF393) renal cancer cells was observed with series 3 compounds, while in the other two series 6 and 8, there was a significant inhibition of ovarian cancer cells (OVCAR-8) and melanoma cells (SK-MEL-2). Interestingly; beside the strong inhibition of compound 3q to IGROV1 and RXF393 cells, a great inhibition (199.62%) for (M14) Melanoma cells was observed at the tested concentration (10 microM). ADME-T and pharmacophore prediction methodology were used to study the antitumor activity of the most active compounds and to identify the structural features required for antitumor activity.
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| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical | |
| pubmed:status |
MEDLINE
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| pubmed:month |
Jun
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| pubmed:issn |
1768-3254
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| pubmed:author | |
| pubmed:copyrightInfo |
Copyright (c) 2010 Elsevier Masson SAS. All rights reserved.
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| pubmed:issnType |
Electronic
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| pubmed:volume |
45
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| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
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| pubmed:pagination |
2516-30
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| pubmed:dateRevised |
2010-11-18
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| pubmed:meshHeading |
pubmed-meshheading:20236733-Antineoplastic Agents,
pubmed-meshheading:20236733-Cell Line, Tumor,
pubmed-meshheading:20236733-Cell Proliferation,
pubmed-meshheading:20236733-Drug Screening Assays, Antitumor,
pubmed-meshheading:20236733-Humans,
pubmed-meshheading:20236733-Hydrophobic and Hydrophilic Interactions,
pubmed-meshheading:20236733-Models, Molecular,
pubmed-meshheading:20236733-Molecular Conformation,
pubmed-meshheading:20236733-Structure-Activity Relationship,
pubmed-meshheading:20236733-Sulfonylurea Compounds
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| pubmed:year |
2010
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| pubmed:articleTitle |
Synthesis and antitumor evaluation of novel cyclic arylsulfonylureas: ADME-T and pharmacophore prediction.
|
| pubmed:affiliation |
Department of Medicinal Chemistry, Faculty of Pharmacy, University of Mansoura, Mansoura 35516, Egypt.
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| pubmed:publicationType |
Journal Article
|