Solid phase combinatorial synthesis of benzothiazoles and evaluation of topoisomerase II inhibitory activity

Suk June Choi, Hyen Joo Park, Sang Kook Lee, Sang Woong Kim, Gyoonhee Han, Hea Young Park Choo

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To investigate one possible mechanism of action of the cytotoxic activity of benzothiazoles, we synthesized 2-(substituted-phenyl)benzothiazoles and evaluated their ability to inhibit topoisomerase II activities. Solid phase combinatorial method using trityl resin was employed and benzothiazole derivatives with various substitution on 2′-, 3′-, or 4′-position of phenyl group were obtained in ca. 30 mg scale (7-96% yield). Most of the compounds synthesized exhibited topoisomerase II inhibitory activity at 100 μM. 2-(3-Amino-4-methylphenyl)benzothiazole showed high activity (IC50 = 71.7 μM), comparable to etoposide (IC 50 = 78.4 μM).

Original languageEnglish
Pages (from-to)1229-1235
Number of pages7
JournalBioorganic and Medicinal Chemistry
Issue number4
Publication statusPublished - 2006 Feb 15


All Science Journal Classification (ASJC) codes

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

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