Potential antitumor agents. 21. Dialkanolamine dialkanesulfonic esters.
Homologous dialkanesulfonic esters of 2,2'-iminodiethanol, 3,3'-iminodi-1-propanol, N-(2-hydroxyethyl)-6-amino-1-hexanol, and N-(3-hydroxypropyl)-6-amino-1-hexanol were prepared via the N-trityl derivatives and screened for L1210 activity. For each active agent significant increases in life-span in L1210 tests (ILS) were correlated by linear least-squares regression with the corresponding log doses. The maximum ILS, taken from this regression line at the determined LD10, was used as a quantitative measure of antileukemic effectivenss. Within each homologoud series log ILSmax could be correlated with a binomial expression in lipophilic-hydrophilic balance, as measured by Rm values, but all active members from the four series could not be successfully included in a single correlation. By modification of Rm values with an ionization factor, log (H+/H+ + Ka), all active compounds could then be included in a significant correlation equation.
D000476:Alkanesulfonates / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D000588:Amines / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000627:therapeutic use; D007939:Leukemia L1210 / Q000188:drug therapy; D008433:Mathematics; D051379:Mice; D008809:Mice, Inbred C3H; D008811:Mice, Inbred DBA; D013329:Structure-Activity Relationship
D000476:Alkanesulfonates; D000588:Amines; D000970:Antineoplastic Agents