rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
6
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pubmed:dateCreated |
2011-3-14
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pubmed:abstractText |
A series of novel bichalcone analogs were synthesized and evaluated in lipopolysaccharide (LPS)-activated microglial cells as inhibitors of nitric oxide (NO) and for in vitro anticancer activity using a limited panel of four human cancer cell lines. All analogs inhibited NO production. Compounds 4 and 11 exhibited optimal activity with IC(50) values of 0.3 and 0.5 ?M, respectively, and were at least 38-fold better than the positive control. A mechanism of action study showed that both compounds significantly blocked the nuclear translocation of NF-?B p65 and up-regulation of iNOS at 1.0 ?M. Compound 4 and three other analogs (3, 20, and 23) exerted significant in vitro anticancer activity GI(50) values ranging from 0.70 to 13.10 ?M. A mode of action study using HT-29 colon cancer cells showed that 23 acts by inducing apoptosis signaling.
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pubmed:grant |
|
pubmed:language |
eng
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pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Mar
|
pubmed:issn |
1464-3391
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pubmed:author |
|
pubmed:copyrightInfo |
Copyright © 2011 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
|
pubmed:volume |
19
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
1895-906
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pubmed:meshHeading |
pubmed-meshheading:21377368-Animals,
pubmed-meshheading:21377368-Antigens, CD95,
pubmed-meshheading:21377368-Antineoplastic Agents,
pubmed-meshheading:21377368-Apoptosis,
pubmed-meshheading:21377368-Cell Line, Tumor,
pubmed-meshheading:21377368-Chalcones,
pubmed-meshheading:21377368-Drug Screening Assays, Antitumor,
pubmed-meshheading:21377368-Humans,
pubmed-meshheading:21377368-Mice,
pubmed-meshheading:21377368-Nitric Oxide,
pubmed-meshheading:21377368-Nitric Oxide Synthase Type II,
pubmed-meshheading:21377368-Pyridines,
pubmed-meshheading:21377368-Transcription Factor RelA
|
pubmed:year |
2011
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pubmed:articleTitle |
New bichalcone analogs as NF-?B inhibitors and as cytotoxic agents inducing Fas/CD95-dependent apoptosis.
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pubmed:affiliation |
Department of Chemistry, National Cheng Kung University, Tainan 701, Taiwan.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't,
Research Support, N.I.H., Extramural
|