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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
11
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pubmed:dateCreated |
1991-12-31
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pubmed:abstractText |
In an attempt to determine some of the structural features of geiparvarin (1) that account for its cytostatic activity in vitro, a series of geiparvarin analogues (10a-i, 1, 12, and 14-16) which contain novel modifications in the region of the olefinic double bond and of the coumarin moiety have been designed and synthesized. Among the derivatives containing a carbamate moiety, only the analogues containing a carbamate group linked to an alkyl moiety 10b-i were endowed with potent cytostatic activity, whereas the corresponding benzene derivative 10a was devoid of any antiproliferative activity. 6-Methoxygeiparvarin 101 proved equally effective as geiparvin (1), while compounds containing an additional double bond at the side chain (12 and 14-16) were invariably 5-100-fold less effective than geiparvarin. Diene derivative 15, bearing a coumarin moiety, was essentially inactive against murine (L1210, FM3A) tumor cells but exhibited good activity against human (Molt/4F, MT-4) tumor 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/Antineoplastic Agents, Phytogenic,
http://linkedlifedata.com/resource/pubmed/chemical/Carbamates,
http://linkedlifedata.com/resource/pubmed/chemical/Coumarins,
http://linkedlifedata.com/resource/pubmed/chemical/Furans,
http://linkedlifedata.com/resource/pubmed/chemical/geiparvarin
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
34
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3172-6
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:1956034-Animals,
pubmed-meshheading:1956034-Antineoplastic Agents, Phytogenic,
pubmed-meshheading:1956034-Carbamates,
pubmed-meshheading:1956034-Coumarins,
pubmed-meshheading:1956034-Furans,
pubmed-meshheading:1956034-Humans,
pubmed-meshheading:1956034-Leukemia L1210,
pubmed-meshheading:1956034-Mice,
pubmed-meshheading:1956034-Stereoisomerism,
pubmed-meshheading:1956034-Structure-Activity Relationship,
pubmed-meshheading:1956034-Tumor Cells, Cultured
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pubmed:year |
1991
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pubmed:articleTitle |
Geiparvarin analogues. 2. Synthesis and cytostatic activity of 5-(4-arylbutadienyl)-3(2H)-furanones and of N-substituted 3-(4-oxo-2-furanyl)-2-buten-2-yl carbamates.
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pubmed:affiliation |
Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Italy.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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