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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
5
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pubmed:dateCreated |
1981-8-10
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pubmed:abstractText |
Factors influencing dose potency of 4'-(9-acridinylamino)methanesulfon-m-anisidide (m-AMSA) analogues in L1210 assays have been investigated by multiple regression analysis. The dependent variable was D40, the dose to provide 40% life extension in L1210 tests. Independent variables examined were chromatographic Rm values, as a measure of agent lipophilic-hydrophilic balance; Rm2; log K, where K is the agent-DNA association constant for poly[d(A-T)]; log T1/2, the half-life for congener thiolytic cleavage; and agent pKa values. A regression equation containing terms in Rm2 and log K was derived with the latter term accepting the greater proportion of the biological variance. DNA binding, of acridine substituted m-AMSA variants, is the most important factor influencing dose potency. Modeling of log K for 3-substituted derivatives provided an equation in substituent R constants and molar refractivities (MR).
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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 |
May
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
24
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
520-5
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pubmed:dateRevised |
2008-11-21
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pubmed:meshHeading |
pubmed-meshheading:6894620-Aminoacridines,
pubmed-meshheading:6894620-Amsacrine,
pubmed-meshheading:6894620-Animals,
pubmed-meshheading:6894620-Antineoplastic Agents,
pubmed-meshheading:6894620-Chemistry, Physical,
pubmed-meshheading:6894620-DNA,
pubmed-meshheading:6894620-Kinetics,
pubmed-meshheading:6894620-Leukemia L1210,
pubmed-meshheading:6894620-Mice,
pubmed-meshheading:6894620-Physicochemical Phenomena,
pubmed-meshheading:6894620-Structure-Activity Relationship
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pubmed:year |
1981
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pubmed:articleTitle |
Potential antitumor agents. 35. Quantitative relationships between antitumor (L1210) potency and DNA binding for 4'-(9-acridinylamino)methanesulfon-m-anisidide analogues.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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