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Synthesis, DNA Binding, and Leishmania Topoisomerase Inhibition Activities of a Novel Series of Anthra[1,2-d]imidazole-6,11-dione Derivatives

IR@IICB: CSIR-Indian Institute of Chemical Biology, Kolkata

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Title Synthesis, DNA Binding, and Leishmania Topoisomerase Inhibition Activities of a Novel Series of Anthra[1,2-d]imidazole-6,11-dione Derivatives
 
Creator Chaudhuri, Padmaparna
Majumder, Hemanta K
Bhattacharya, Santanu
 
Subject Infectious Diseases and Immunology
 
Description Leishmania donoVani, a unicellular kinetoplastid protozoan parasite, is the causative agent for human visceral leishmaniasis, which is a fatal disease affecting the liver and spleen. It has currently been listed by the World Health Organization as the second most important protozoan disease after malaria in terms of patient mortalities and is prevalent in many tropical countries.1 Treatment of leishmaniasis depends entirely upon chemotherapy, yet the available range of effective drugs is highly limited.1 In an attempt to identify new molecular targets for antiparasitic drugs, attention has been focused on DNA topoisomerases,2 a class of enzymes playing critical roles in virtually every aspect of DNA metabolism.3,4 Herein, we report a series of new small molecules, some of which have emerged as potent inhibitors of topoisomerase I (topo I) of parasitic pathogen Leishmania donoVani.
 
Date 2007
 
Type Article
PeerReviewed
 
Format application/pdf
 
Identifier http://www.eprints.iicb.res.in/348/1/JOURNAL_OF_MEDICINAL_CHEMISTRY%2C50(_10)%2C_2536%2D2540_[85].pdf
Chaudhuri, Padmaparna and Majumder, Hemanta K and Bhattacharya, Santanu (2007) Synthesis, DNA Binding, and Leishmania Topoisomerase Inhibition Activities of a Novel Series of Anthra[1,2-d]imidazole-6,11-dione Derivatives. Journal of Medicinal Chemistry, 50 (10). pp. 2536-2540.
 
Relation http://dx.doi.org/10.1021/jm0610604
http://www.eprints.iicb.res.in/348/