当前位置： SCI文献检索 > JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Potential antitumor agents. 35. Quantitative relationships between antitumor (L1210) potency and DNA binding for 4'-(9-acridinylamino)methanesulfon-m-anisidide analogues.

Potential antitumor agents. 35. Quantitative relationships between antitumor (L1210) potency and DNA binding for 4'-(9-acridinylamino)methanesulfon-m-anisidide analogues.

Abstract：

: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).

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Baguley BC,Denny WA,Atwell GJ,Cain BF

doi

10.1021/jm00137a009

subject

Has Abstract

pub_date

1981-05-01 00:00:00

pages

520-5

issue

5

eissn

0022-2623

issn

1520-4804

journal_volume

24

pub_type

杂志文章

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