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

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Konuş M., Kıvrak A., Yılmaz C., Arslan Ş., Kurt Kızıldoğan A., Çetin D., ...More

Letters In Drug Design & Discovery, vol.18, no.5, pp.461-470, 2021 (Peer-Reviewed Journal)

  • Publication Type: Article / Article
  • Volume: 18 Issue: 5
  • Publication Date: 2021
  • Doi Number: 10.2174/1570180817999201109203226
  • Journal Name: Letters In Drug Design & Discovery
  • Journal Indexes: Science Citation Index Expanded, Scopus, Biotechnology Research Abstracts, Chemical Abstracts Core, EMBASE
  • Page Numbers: pp.461-470


Abstract: A novel 1-ethyl-2-phenyl-3-(phenylethynyl)-1H-indole (EPI) derivative was synthesized by electrophilic aromatic substitution reaction and Pd-catalyst Sonogashira coupling reactions. In this study, we found that 1-ethyl-2-phenyl-3-(phenylethynyl)-1H-indole showed significant reducing activity and a broad range of antimicrobial activity. Moreover, 1-ethyl-2-phenyl-3- (phenylethynyl)-1H-indole displayed significant induction in glutathione S-transferases (GST) enzyme activity in human liver cancer cell lines (HepG2), but the cytotoxic effect on all tested cancer cell lines could not be observed. 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.