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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
9
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pubmed:dateCreated |
1990-10-4
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pubmed:abstractText |
A versatile and efficient synthetic route to 4-demethoxyanthracyclinones has been utilized in the preparation of a number of aglycons having 9-alkyl, 9-(hydroxylalkyl), or 9-carbamoyl substituents. Silver trifluoromethanesulfonate catalyzed coupling of these aglycons with various daunosamine derivatives has yielded a series of novel anthracyclines which have been evaluated as antitumor agents. 9-Alkylanthracyclines 22, 23, 33, and 34 have higher efficacy vs L-1210 leukemia than the parent 4-demethoxydaunorubicin (21), or the natural anthracyclines daunorubicin (1) and doxorubicin (2). 9-(Hydroxyalkyl) derivatives have in most cases high efficacy but are slightly less potent than 21. 9-Methyl analogue 22 has higher efficacy vs P388 leukemia than other anthracyclines tested, while 9-(hydroxymethyl) derivative 37 retains similar efficacy to anthracyclines 1, 2, and 21 but is considerably more potent. The N-substituted 9-carbamoylanthracyclines are devoid of antitumor activity.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
33
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2375-9
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pubmed:dateRevised |
2008-11-21
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pubmed:meshHeading |
pubmed-meshheading:2391681-Animals,
pubmed-meshheading:2391681-Antibiotics, Antineoplastic,
pubmed-meshheading:2391681-Chemical Phenomena,
pubmed-meshheading:2391681-Chemistry,
pubmed-meshheading:2391681-Doxorubicin,
pubmed-meshheading:2391681-Female,
pubmed-meshheading:2391681-Idarubicin,
pubmed-meshheading:2391681-Leukemia L1210,
pubmed-meshheading:2391681-Leukemia P388,
pubmed-meshheading:2391681-Mice,
pubmed-meshheading:2391681-Structure-Activity Relationship
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pubmed:year |
1990
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pubmed:articleTitle |
Synthesis and antitumor activity of novel 4-demethoxyanthracyclines.
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pubmed:affiliation |
Roche Products Limited, Welwyn Garden City, Hertfordshire, England.
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pubmed:publicationType |
Journal Article
|