Source:http://linkedlifedata.com/resource/pubmed/id/18346898
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
8
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pubmed:dateCreated |
2008-4-24
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pubmed:abstractText |
As part of our continuing search for potential differentiation agents, 1-benzyl-3-(4-pyridinylmethylidenyl)indolin-2-one (14) was selected as lead compound, and its new pyridinyl and quinolinyl analogs were synthesized and evaluated for differentiation-inducing activity toward HL-60 cells. Most of the tested compounds enhanced the ATRA-induced differentiation; among them, 1-(1-phenylethyl)-3-(3-quinolinylmethylidenyl)indolin-2-one (25) was the most promising one. The two isomers, 25Z and 25E; consisting 25 were found to have similar differentiation activity. The combination of 25 with all trans retinoic acid (ATRA) was found to induce complete differentiation of HL-60 cells and arrest the cells in the G(0)/G(1) phase of the cell cycle. Beside its excellent differentiation activity, 25 also exhibited relatively low cytotoxicity toward normal cells. Therefore, compound 25 is recommended as a candidate for further development of novel enhancer of ATRA-induced differentiation in HL-60 cells.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Pyrimidines,
http://linkedlifedata.com/resource/pubmed/chemical/Quinolines,
http://linkedlifedata.com/resource/pubmed/chemical/Tretinoin,
http://linkedlifedata.com/resource/pubmed/chemical/pyrimidine,
http://linkedlifedata.com/resource/pubmed/chemical/quinoline
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
1464-3391
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
16
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4222-32
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pubmed:meshHeading |
pubmed-meshheading:18346898-Cell Differentiation,
pubmed-meshheading:18346898-Cell Proliferation,
pubmed-meshheading:18346898-Cell Shape,
pubmed-meshheading:18346898-HL-60 Cells,
pubmed-meshheading:18346898-Humans,
pubmed-meshheading:18346898-Magnetic Resonance Spectroscopy,
pubmed-meshheading:18346898-Methylation,
pubmed-meshheading:18346898-Molecular Structure,
pubmed-meshheading:18346898-Pyrimidines,
pubmed-meshheading:18346898-Quinolines,
pubmed-meshheading:18346898-Structure-Activity Relationship,
pubmed-meshheading:18346898-Tretinoin
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pubmed:year |
2008
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pubmed:articleTitle |
Synthesis of 1-substituted 3-pyridinylmethylidenylindolin-2-ones and 1-substituted 3-quinolinylmethylidenylindolin-2-ones as the enhancers of ATRA-induced differentiation in HL-60 cells.
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pubmed:affiliation |
Biomedical Engineering Center, Industrial Technology Research Institute, Hsinchu, Taiwan.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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