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Bioorg Med Chem
; 14(4): 1229-35, 2006 Feb 15.
Article
in English
| MEDLINE
| ID: mdl-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).