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2007 | 54 | 3 | 561-565
Article title

1H-Benzimidazole derivatives as mammalian DNA topoisomerase I inhibitors

Content
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EN
Abstracts
EN
Benzimidazole is one of the most important heterocyclic groups manifesting various biological properties, such as antibacterial, antifungal, antimicrobial, antiprotozoal and antihelmintic activities. Several benzimidazole derivatives are also active as inhibitors of type I DNA topoisomerases. In this study, three 1H-benzimidazole derivatives with different electronic characteristics at position 5-, namely 5-chloro-4-(1H-benzimidazole-2-yl)phenol (Cpd I), 5-methyl-4-(1H-benzimidazole-2-yl)phenol (Cpd II) and 4-(1H-benzimidazole-2-yl)phenol (Cpd III), were synthesized and evaluated for their effects on mammalian type I DNA topoisomerase activity using quantitative in vitro plasmid supercoil relaxation assays. For the structure elucidation of the compounds, melting points, UV, IR, 1H NMR, 13C NMR, mass spectral data and elemental analyses were interpreted. Among the compounds, 5-methyl-4-(1H-benzimidazole-2-yl)phenol (Cpd II) manifested relatively potent topoisomerase I inhibition.
Publisher

Year
Volume
54
Issue
3
Pages
561-565
Physical description
Dates
published
2007
received
2007-03-14
revised
2007-07-30
accepted
2007-08-28
(unknown)
2007-09-06
Contributors
  • Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ege University, Izmir, Turkey
author
  • Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ege University, Izmir, Turkey
author
  • Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Ege University, Izmir, Turkey
References
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Document Type
Publication order reference
Identifiers
YADDA identifier
bwmeta1.element.bwnjournal-article-abpv54p561kz
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