Abstract
We have designed and synthesized a series of 2,4,6-triaryl pyridine derivatives containing chlorophenyl and phenolic moeity at 2- and 4- position of the central pyridine, respectively, resulting in a total of 42 compounds. They were evaluated for topoisomerase I and II inhibitory activities as well as cytotoxicities against several human cancer cell lines. Most compounds showed better topoisomerase II inhibitory activity compared to topoisomerase I inhibitory activity. Compounds 19, 20, 26-28, and 47-50 especially showed stronger topo II inhibitory activity than etoposide.
Copyright © 2012 Elsevier Masson SAS. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry*
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Antineoplastic Agents / pharmacology*
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Cell Line, Tumor
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Chemistry Techniques, Synthetic*
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DNA Topoisomerases, Type I / chemistry
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DNA Topoisomerases, Type I / metabolism
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DNA Topoisomerases, Type II / chemistry
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DNA Topoisomerases, Type II / metabolism
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Drug Design*
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Humans
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Models, Molecular
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Phenols / chemistry*
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Protein Conformation
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Pyridines / chemical synthesis
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Pyridines / chemistry*
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Pyridines / pharmacology*
Substances
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Antineoplastic Agents
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Phenols
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Pyridines
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DNA Topoisomerases, Type I
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DNA Topoisomerases, Type II