Isobrassinin and its analogues: Novel types of antiproliferative agents

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29 Citations (Scopus)

Abstract

Isobrassinin (2-(S-methyldithiocarbamoylaminomethyl)indole (7a), a regioisomer of the cruciferous phytoalexin brassinin (1), exerted marked antiproliferative effects on the HeLa, A431 and MCF7 cell lines (>78.6% inhibition at 30 μM). For structure-activity relationships, further analogues were synthesized. The highest cytotoxic effect was displayed by 2-phenylimino-1,3-thiazino[5,6-b]indole (10) (10 μM, 76.8%-HeLa and 46.3%-MCF7). The effect of the natural phytoalexin brassinin was also determined.

Original languageEnglish
Pages (from-to)6273-6276
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number24
DOIs
Publication statusPublished - Dec 15 2006

Keywords

  • 2-Aminomethylindole
  • Antitumour activity
  • Dithiocarbamate
  • Thiazino[5,6-b]indole

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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