S. Ray et al., DUAL INHIBITION OF DNA TOPOISOMERASES OF LEISHMANIA-DONOVANI BY NOVELINDOLYL QUINOLINES, Biochemical and biophysical research communications, 230(1), 1997, pp. 171-175
A wide variety of biologically active compounds contain indole and qui
noline nuclei. A one step synthesis of some novel indolyl quinoline an
alogs e.g. 2-(2 Dichloro-acetamidobenzyl)-3-(3'-indolyl)-quinoline [1]
, 2-(2 ''-Dichloroacetamido-5 ''-bromobenzyl)-3'-[3'-(5'-bromoindolyl)
]-6-bromo quinoline [2], and 2-(2 ''-acetamido benzyl)-3-(3'-indolyl)-
quinoline [3] has been developed under Friedel-Crafts acylation condit
ions. The compounds inhibit the relaxation and decatenation reactions
catalysed by type I and type II DNA topoisomerases of Leishmania donov
ani. Among the three synthetic indolyl quinolines, the Br-derivative [
2] is most active, The results reported here concerning the inhibition
of type I and type II DNA topoisomerases indicate that the compounds
act as ''dual inhibitors'' of the enzymes and can be exploited for rat
ional drug design in human leishmaniasis. (C) 1997 Academic Press