TY - JOUR
T1 - Dual inhibition of DNA topoisomerases of Leishmania donovani by novel indolyl quinolines
AU - Ray, Sutapa
AU - Sadhukhan, Pranab K.
AU - Mandal, Nirup B.
AU - Mahato, Sashi B.
AU - Majumder, Hemanta K.
N1 - Funding Information:
We thank Dr. J. Das, The Director and Prof. A. N. Bhaduri, The Ex-Director of this Institute for their interest in this work. The ®nancial support from Council of Scienti®c and Industrial Research, India in the form of Senior Research Fellowship to S. Ray and in the form of Emeritus Scientist to S. B. Mahato are gratefully acknowledged. We also thank the Department of Biotechnology for Research support.
PY - 1997/1/3
Y1 - 1997/1/3
N2 - 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.
AB - 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.
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U2 - 10.1006/bbrc.1996.5874
DO - 10.1006/bbrc.1996.5874
M3 - Article
C2 - 9020039
AN - SCOPUS:0031550251
SN - 0006-291X
VL - 230
SP - 171
EP - 175
JO - Biochemical and Biophysical Research Communications
JF - Biochemical and Biophysical Research Communications
IS - 1
ER -