Potential antitumor agents. 21. Dialkanolamine dialkanesulfonic esters

Abstract

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 [mouse leukemia] 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 effectiveness. Within each homologous 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 4 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.