The Effect of 5-Substitution on the Cytotoxicity of 2-(p-Methoxyphenyl)-1H-Benzimidazoles in Human Cancer Cell Lines

Min Jin Kwon; Hwan Mook Kim; Dae Duk Kim; Jung Sun Kim

doi:10.4028/www.scientific.net/KEM.277-279.23

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HomeKey Engineering MaterialsKey Engineering Materials Vols. 277-279The Effect of 5-Substitution on the Cytotoxicity...

The Effect of 5-Substitution on the Cytotoxicity of 2-(p-Methoxyphenyl)-1H-Benzimidazoles in Human Cancer Cell Lines

Abstract:

A series of 5-substituted 2-(p-methoxyphenyl)-1H-benzimidazoles was synthesized and evaluated for cytotoxicity against 4 human cancer cell lines, HCT 15, PC-3, A549, and ACHN. Except for the 5-chloro analogue, most of the 5-substituted compounds showed significant cytotoxicities in these cell lines. However, the structure activity relationship study revealed that neither the electronic nor the lipophilic parameters of the 5-substituents were related to cytotoxicity. Moreover, none of the analogues showed significant NF к-β inhibition activity implying that cytotoxicity was not related to this mechanism. The 5-methyl analogue was the most potent compound in this series with a GI50 of 0.9 µM in the A549 cell line.

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Key Engineering Materials (Volumes 277-279)

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23-27

DOI:

https://doi.org/10.4028/www.scientific.net/KEM.277-279.23

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Online since:

January 2005

Authors:

Min Jin Kwon, Hwan Mook Kim, Dae Duk Kim, Jung Sun Kim

Keywords:

2-(p-Methoxyphenyl)-1H-Benzimidazole, Cytotoxicity, NFK-β Inhibition, Structure Activity Relationship

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