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Title 

The effect of 5-substitution on the cytotoxicity of 2-(p-methoxyphenyl)-1H-benzimidazoles in human cancer cell lines

Authors 

M J KwonHwan Mook KimD D KimJ S Kim

Publisher 

Trans Tech Publications

Issue Date 

2005

Citation 

Key Engineering Materials, vol. 277, no. 1, pp. 23-27

Keywords 

2-(p-methoxyphenyl)-1h-benzimidazolecytotoxicityNF K-β inhibitionstructure activity relationshipsubstitution reactionssynthesis (chemical)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 K-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.

ISSN 

1013-9826

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2017-04-19


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