Dual inhibition of DNA topoisomerases of Leishmania donovaniby novel indolyl quinolines

Ray, Sutapa ; Sadhukhan, Pranab K. ; Mandal, Nirup B. ; Mahato, Sashi B. ; Majumder, Hemanta K. (1997) Dual inhibition of DNA topoisomerases of Leishmania donovaniby novel indolyl quinolines Biochemical and Biophysical Research Communications, 230 (1). pp. 171-175. ISSN 0006-291X

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Official URL: http://www.sciencedirect.com/science/article/pii/S...

Related URL: http://dx.doi.org/10.1006/bbrc.1996.5874

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 ofLeishmania 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.

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