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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Research Article

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

Author(s): Aslıhan Kurt-Kızıldoğan, Çiğdem Otur, Can Yılmaz, Sevki Arslan, Dogukan Mutlu, Arif Kivrak*, Muheb Algso, Abdussamet Kayhan, Doğan Çetin and Metin Konus*

Volume 18, Issue 5, 2021

Published on: 09 November, 2020

Page: [461 - 470] Pages: 10

DOI: 10.2174/1570180817999201109203226

Price: $65


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.

Graphical Abstract
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