Design, synthesis and biological evaluation of novel 5-bromo derivatives of indole phytoalexins

  1. Mariana BudovskáORCID Logo,
  2. Ivana Selešová,
  3. Viera Tischlerová,
  4. Radka Michalková and
  5. Ján MojžišORCID Logo

Submitting author affiliation: Faculty of Science, Pavol Jozef Šafárik University in Košice, Košice, Slovakia

Beilstein Arch. 2020, 202023.

Published 05 Mar 2020

  • Preprint


The increasing diversity of small molecule libraries is a major source for the discovery of new drug candidates. In term of this trend, we report the synthesis five series 5-bromosubstituted derivatives of indole phytoalexins Type A-E using straightforward synthetic approach. Novel compounds were screened in vitro for antiproliferative/cytotoxic activity against seven human cancer cell lines by MTT assay. Evaluation of their antiproliferative potency showed that the activity of some analogues was better or comparable to that of cisplatin and at the same time the toxicity of these compounds on 3T3 cells was lower than that of cisplatin. We found that all 5-bromosubstituted analogues of indole phytoalexins Type A-E exhibited lower or approximately the same activities as a previously studied corrensponding non-brominated compounds.

Keywords: 5-bromobrassinin; indole; phytoalexins; cyclization reactions; antiproliferative activity

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Budovská, M.; Selešová, I.; Tischlerová, V.; Michalková, R.; Mojžiš, J. Beilstein Arch. 2020, 202023. doi:10.3762/bxiv.2020.23.v1

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