Source:http://linkedlifedata.com/resource/pubmed/id/19013820
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
24
|
| pubmed:dateCreated |
2008-11-25
|
| pubmed:abstractText |
A series of novel pyrazolo[1,5-a]pyrazin-4(5H)-one derivatives were synthesized by the reaction of ethyl 3-aryl-1-(2-bromoethyl)-1H-pyrazole-5-carboxylate and amine in the general heating condition and microwave-assisted condition. The structures of the compounds were determined by IR, (1)H NMR and mass spectroscopy, in addition, representative single-crystal structures were characterized by using X-ray diffraction analysis. Preliminary biological evaluation showed that the compounds could inhibit the growth of A549 cells in dosage- and time-dependent manners. The study on structure-activity relationships showed that compounds with 4-chlorophenyl group at pyrazole moiety, such as 5-benzyl-2-(4-chlorophenyl)-6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one (3o) had much more inhibitory effects. Compound 3o was the most effective small molecule in inhibiting A549 cell growth and might perform its action through modulating autophagy.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:month |
Dec
|
| pubmed:issn |
1464-3391
|
| pubmed:author | |
| pubmed:issnType |
Electronic
|
| pubmed:day |
15
|
| pubmed:volume |
16
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
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| pubmed:pagination |
10165-71
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| pubmed:meshHeading |
pubmed-meshheading:19013820-Antineoplastic Agents,
pubmed-meshheading:19013820-Cell Line, Tumor,
pubmed-meshheading:19013820-Crystallography, X-Ray,
pubmed-meshheading:19013820-DNA Damage,
pubmed-meshheading:19013820-Drug Design,
pubmed-meshheading:19013820-Drug Screening Assays, Antitumor,
pubmed-meshheading:19013820-Humans,
pubmed-meshheading:19013820-Inhibitory Concentration 50,
pubmed-meshheading:19013820-Lung Neoplasms,
pubmed-meshheading:19013820-Molecular Structure,
pubmed-meshheading:19013820-Pyrazoles,
pubmed-meshheading:19013820-Structure-Activity Relationship
|
| pubmed:year |
2008
|
| pubmed:articleTitle |
Synthesis and preliminary biological evaluation of novel pyrazolo[1,5-a]pyrazin-4(5H)-one derivatives as potential agents against A549 lung cancer cells.
|
| pubmed:affiliation |
Institute of Organic Chemistry, School of Chemistry and Chemical Engineering, Shandong University, Jinan 250100, PR China.
|
| pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|