Synthesis, Cytotoxicity, Antioxidant and Antimicrobial Activity of Indole Based Novel Small Molecules

Aslıhan       Kurt-Kızıldoğan; Çiğdem       Otur; Can       Yılmaz; Sevki       Arslan; Dogukan       Mutlu; Arif       Kivrak; Muheb       Algso; Abdussamet       Kayhan; Doğan       Çetin; Metin       Konus

doi:10.2174/1570180817999201109203226

Abstract

Aims: In this study experiments were carried out to explore antioxidant, antimicrobial, cytotoxic properties of novel indole derivative 1-ethyl-2-phenyl-3-phenylethyl-3-thiophen-2-yl-1Hindole (EPI) together with its effect on glutathione S-transferases (GST) activities in human liver carcinoma (HepG2) cells.

Background: Indoles probably represent one of the most important heterocyclic structures that have been attracting the interest of many scientists in drug discovery.

Objective: The present study was carried out to explore antioxidant, antimicrobial, cytotoxic properties of novel indole derivative 1-ethyl-2-phenyl-3-phenylethyl-3-thiophen-2-yl-1H-indole (EPI) and its effect on glutathione S-transferases (GST) activities in human liver carcinoma (HepG2) cells.

Materials and Methods: Pd-catalyst Sonogashira coupling reactions, MTT Assay, Antioxidant capacity test, Antimicrobial test, GST enzyme activity test.

Results: 1-ethyl-2-phenyl-3-(phenylethynyl)-1H-indole had antioxidant and antimicrobial properties. It displayed significant induction in glutathione S-transferases (GST) enzyme activity in human liver cancer cell lines (HepG2), but cytotoxic effect on all tested cancer cell lines could not be observed.

Conclusion: All of these results showed that 1-ethyl-2-phenyl-3-(phenylethynyl)-1H-indole had antioxidant and antimicrobial properties without cytotoxic effect, which could make it a promising active component with further studies.

Keywords: Indole, heteroaromatic compounds, antioxidant, cytotoxicity, antimicrobial, small molecules.

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DOI https://dx.doi.org/10.2174/1570180817999201109203226	Print ISSN 1570-1808
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Synthesis, Cytotoxicity, Antioxidant and Antimicrobial Activity of Indole Based Novel Small Molecules

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