Synthesis, DNA binding, and leishmania topoisomerase inhibition activities of a novel series of anthra[1,2-d]imidazole-6,11-dione derivatives

Chaudhuri, Padmaparna ; Majumder, Hemanta K. ; 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. ISSN 0022-2623

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Official URL: http://pubs.acs.org/doi/abs/10.1021/jm0610604

Related URL: http://dx.doi.org/10.1021/jm0610604

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 IC50~ 1 μM. The inhibition activities were not related with their DNA binding affinity and depended on the nature of the side chain.

Item Type:Article
Source:Copyright of this article belongs to American Chemical Society.
ID Code:20948
Deposited On:20 Nov 2010 13:17
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