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

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. In: Journal of Medicinal Chemistry, 50 (10). pp. 2536-2540.

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Abstract

Nine novel anthra[1,2-d]imidazole-6,11-diones, differing in their side chain, were synthesized. UV-vis spectroscopy and viscometric titrations of these molecules with duplex DNA were used to assess their binding with DNA. Five of the nine compounds showed high inhibition activity against topoisomerase I of Leishmania donoVani, with the one bearing the tetrazole side chain exhibiting an $IC_{50}$ $\sim 1 \mu M$. The inhibition activities were not related with their DNA binding affinity and depended on the nature of the side chain.

Item Type:	Journal Article
Publication:	Journal of Medicinal Chemistry
Publisher:	American Chemical Society
Additional Information:	Copyright of this article belongs to American Chemical Society.
Department/Centre:	Division of Chemical Sciences > Organic Chemistry
Date Deposited:	13 Jul 2007
Last Modified:	27 Jan 2012 06:15
URI:	http://eprints.iisc.ac.in/id/eprint/11544

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