Some characteristics of activity of potential chemotherapeutics--benzimidazole derivatives

Advances in Medical Sciences
Katarzyna Błaszczak-Świątkiewicz, Elżbieta Mikiciuk-Olasik

Abstract

In this work, the biological activity of some benzimidazoles and benzimidazole-4,7-diones was compared. These two groups of compounds were evaluated as potential chemotherapeutics and their characteristic relationship structure to biological activity was discussed. The authors compared their effect into the cytotoxic, apoptosis and DNA destruction approach. Their cytotoxic effect on the human lung adenocarcinoma A549 cells line was determined by WST-1 test. Next the cytotoxic way of tumor cells death was determined by caspase 3/7 test. The last point referred to the DNA destruction of A549 cells and test in situ DNA Assay Kit was applied. Two of the examined compounds (B2 and D2) show a very good correlation of the cytotoxic effect normoxia to hypoxia and they have been found as the potential agents of the DNA damage. The most cytotoxic feature possesses N-oxide benzimidazole derivatives (D and B groups). The screening test of the DNA damage established that N-oxide benzimidazole derivatives (D and B groups) can be more potent as the hypoxia-selective agents for tumor cells than benzimidazole derivatives (A and C groups). Additionally, the test of the caspase-dependent apoptosis proved that the exposure of benzimidazole-4,7-dio...Continue Reading

References

Apr 27, 2000·Bioorganic & Medicinal Chemistry Letters·S JinE J LaVoie
Sep 30, 2000·Bioorganic & Medicinal Chemistry Letters·L GarutiM Castelli
Mar 22, 2002·The Lancet Oncology·W A Denny
Apr 20, 2004·Archiv der Pharmazie·Elzbieta Mikiciuk-OlasikTadeusz J Bartczak
Jul 21, 2004·Il Farmaco·Laura GarutiSilvana Hrelia
Aug 7, 2007·Journal of Medicinal Chemistry·Masaichi HasegawaMui Cheung
May 25, 2011·Nature Reviews. Cancer·William R Wilson, Michael P Hay
Jun 7, 2014·Pharmacological Reports : PR·Katarzyna Błaszczak-ŚwiątkiewiczElżbieta Mikiciuk-Olasik

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Citations

May 24, 2016·Archiv der Pharmazie·Olayinka O AjaniIfedolapo O Olanrewaju

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