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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4
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pubmed:dateCreated |
1987-5-11
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pubmed:abstractText |
Structure-activity relationships for a series of acridine-substituted 3'-N(CH3)2 derivatives of the clinical antileukemic drug amsacrine (1) are reported. The parent (unsubstituted) compound 3 has activity against the Lewis lung solid tumor that is superior to amsacrine (1), the new clinical amsacrine analogue 4, and the recently developed 3'-NHCH3 derivative 2. Although the compounds generally bind less well to DNA and are less dose potent in vivo than either their amsacrine (3'-OCH3) or 3'-NHCH3 analogues, they show very high levels of antitumor activity, with the 4-OCH3 derivative capable of effecting 100% cures of the Lewis lung solid tumor. The broad structure-activity relationships for acridine substitution more closely resemble those of the amsacrine than the 3'-NHCH3 series, with 4-substituted and 4,5-disubstituted compounds showing the highest 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 |
Apr
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
30
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
652-8
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pubmed:dateRevised |
2008-11-21
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pubmed:meshHeading |
pubmed-meshheading:3560159-Amsacrine,
pubmed-meshheading:3560159-Animals,
pubmed-meshheading:3560159-Antineoplastic Agents,
pubmed-meshheading:3560159-Carcinoma,
pubmed-meshheading:3560159-Cell Line,
pubmed-meshheading:3560159-Chemical Phenomena,
pubmed-meshheading:3560159-Chemistry,
pubmed-meshheading:3560159-Colonic Neoplasms,
pubmed-meshheading:3560159-DNA,
pubmed-meshheading:3560159-Humans,
pubmed-meshheading:3560159-Leukemia, Experimental,
pubmed-meshheading:3560159-Lung Neoplasms,
pubmed-meshheading:3560159-Mice,
pubmed-meshheading:3560159-Oxidation-Reduction,
pubmed-meshheading:3560159-Structure-Activity Relationship
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pubmed:year |
1987
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pubmed:articleTitle |
Potential antitumor agents. 48. 3'-Dimethylamino derivatives of amsacrine: redox chemistry and in vivo solid tumor activity.
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pubmed:publicationType |
Journal Article,
Comparative Study
|