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

SJ Choi, HJ Park, SK Lee, SW Kim, G Han…

Index: Choi, Suk-June; Park, Hyen Joo; Lee, Sang Kook; Kim, Sang Woong; Han, Gyoonhee; Choo, Hea-Young Park Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 4 p. 1229 - 1235

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Citation Number: 81

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. 30mg scale (7–96% yield). Most of the ...