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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
9
|
pubmed:dateCreated |
1987-10-9
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pubmed:abstractText |
Study of a series of aniline-substituted 9-anilinoacridines related to the antileukemic drug amsacrine showed that a 1'-carbamate group provided increased activity against the multidrug-resistant P388/ADR leukemia subline in vivo. Since activity against such resistant tumors is of great clinical significance, a series of acridine-substituted carbamate derivatives were evaluated against both wild-type and ADR/resistant P388 leukemia and the Lewis lung solid tumor in vivo. Structure-activity relationships for all three tumor lines were similar, with 3-halo-5-methyl and 3-halo-5-methoxy compounds proving the most active. This substitution pattern also provided the highest DNA binding. Such compounds (particularly the 3-chloro-5-methyl and 3-chloro-5-methoxy) have in vivo activity against wild-type P388 and Lewis lung comparable to that of the best amsacrine analogues previously developed (greater than 50% cures), as well as P388/ADR activity. This work essentially completes the development of the amsacrine series of antitumor agents.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Sep
|
pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
|
pubmed:volume |
30
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
1576-81
|
pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:3625706-Amsacrine,
pubmed-meshheading:3625706-Animals,
pubmed-meshheading:3625706-Antineoplastic Agents,
pubmed-meshheading:3625706-Cell Line,
pubmed-meshheading:3625706-Doxorubicin,
pubmed-meshheading:3625706-Drug Resistance,
pubmed-meshheading:3625706-Leukemia, Experimental,
pubmed-meshheading:3625706-Leukemia P388,
pubmed-meshheading:3625706-Structure-Activity Relationship
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pubmed:year |
1987
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pubmed:articleTitle |
Potential antitumor agents. 52. Carbamate analogues of amsacrine with in vivo activity against multidrug-resistant P388 leukemia.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|