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  • Title: Solid phase combinatorial synthesis of benzothiazoles and evaluation of topoisomerase II inhibitory activity.
    Author: Choi SJ, Park HJ, Lee SK, Kim SW, Han G, Choo HY.
    Journal: Bioorg Med Chem; 2006 Feb 15; 14(4):1229-35. PubMed ID: 16242334.
    Abstract:
    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 microM. 2-(3-Amino-4-methylphenyl)benzothiazole showed high activity (IC(50) = 71.7 microM), comparable to etoposide (IC(50) = 78.4 microM).
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