The Effect of 5-Substitution on the Cytotoxicity of 2-(p-Methoxyphenyl)-1H-Benzimidazoles in Human Cancer Cell Lines |
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| Journal | Key Engineering Materials (Volumes 277 - 279) |
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| Volume | On the Convergence of Bio-, Information-, Enrivonmental-, Energy-, Space- and Nano-Technolgies |
| Edited by | Kwang Hwa Chung, Yong Hyeon Shin, Sue-Nie Park, Hyun Sook Cho, Soon-Ae Yoo, Byung Joo Min, Hyo-Suk Lim and Kyung Hwa Yoo |
| Pages | 23-27 |
| DOI | 10.4028/www.scientific.net/KEM.277-279.23 |
| Citation | Min Jin Kwon et al., 2005, Key Engineering Materials, 277-279, 23 |
| 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 |
| 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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