期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 50, 期 10, 页码 2536-2540出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm0610604
关键词
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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 mu M. The inhibition activities were not related with their DNA binding affinity and depended on the nature of the side chain.
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