Dual inhibition of DNA topoisomerases of Leishmania donovani by novel indolyl quinolines

Sutapa Ray, Pranab K. Sadhukhan, Nirup B. Mandal, Sashi B. Mahato, Hemanta K. Majumder

Research output: Contribution to journalArticlepeer-review

37 Scopus citations

Abstract

A wide variety of biologically active compounds contain indole and quinoline nuclei. A one step synthesis of some novel indolyl quinoline analogs e.g. 2-(2'-Dichloro-acetamidobenzyl)-3-(3' -indolyl)quinoline [1], 2-(2'-Dichloroacetamido-5'-bromo- benzyl)-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 conditions. The compounds inhibit the relaxation and decatenation reactions catalysed by type I and type II DNA topoisomerases of Leishmania donovani. 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 rational drug design in human leishmaniasis.

Original languageEnglish (US)
Pages (from-to)171-175
Number of pages5
JournalBiochemical and Biophysical Research Communications
Volume230
Issue number1
DOIs
StatePublished - Jan 3 1997
Externally publishedYes

ASJC Scopus subject areas

  • Biophysics
  • Biochemistry
  • Molecular Biology
  • Cell Biology

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