1H-benzimidazole derivatives as mammalian DNA topoisomerase I inhibitors

• Autorzy: Alpan A. S. , Gunes H.S. , Topcu Z.
• Języki publikacji: EN

Abstrakty

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.

Słowa kluczowe

EN

antifungal activity; antiprotozoal activity; plasmid supercoil relaxation assay; mammal; type I DNA topoisomerase; antibacterial activity; heterocyclic group; benzimidazole; antimicrobial activity; 1H-benzimidazole derivative; antihelmintic activity

• Wydawca: -
• Czasopismo: Acta Biochimica Polonica
• Rocznik: 2007
• Tom: 54
• Numer: 3
• Opis fizyczny: p.561-565,fig.,ref.

Twórcy

autor

Alpan A. S.

• Ege University, 35100, Izmir, Turkey

autor

Gunes H.S.

autor

Topcu Z.

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