1H-Benzimidazole derivatives as mammalian DNA topoisomerase I inhibitors

• Authors: A Selcen Alpan , H Semih Gunes , Zeki Topcu
• Languages of publication: 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.

Keywords

EN

1H-benzimidazole derivatives; type I DNA topoisomerase; plasmid supercoil relaxation assays

• Publisher: Polish Biochemical Society
• Journal: Acta Biochimica Polonica
• Year: 2007
• Volume: 54
• Issue: 3
• Pages: 561-565

Dates

published

2007

received

2007-03-14

revised

2007-07-30

accepted

2007-08-28

(unknown)

2007-09-06

Contributors

author

A Selcen Alpan

• Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ege University, Izmir, Turkey

author

H Semih Gunes

• Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ege University, Izmir, Turkey

author

Zeki Topcu

• Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Ege University, Izmir, Turkey

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