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

Title
Solid phase combinatorial synthesis of benzothiazoles and evaluation of topoisomerase II inhibitory activity
Authors
Choi S.-J.Park H.J.Lee S.K.Kim S.W.Han G.Choo H.-Y.P.
Ewha Authors
박혜영이상국
SCOPUS Author ID
박혜영scopus
Issue Date
2006
Journal Title
Bioorganic and Medicinal Chemistry
ISSN
0968-0896JCR Link
Citation
vol. 14, no. 4, pp. 1229 - 1235
Indexed
SCI; SCIE; SCOPUS WOS scopus
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 μM. 2-(3-Amino-4-methylphenyl)benzothiazole showed high activity (IC50 = 71.7 μM), comparable to etoposide (IC 50 = 78.4 μM). © 2005 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmc.2005.09.051
Appears in Collections:
약학대학 > 약학과 > Journal papers
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