Anadolu University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, 26470 Eskişehir, Turkey.
Eur J Med Chem. 2010 Aug;45(8):3320-8. doi: 10.1016/j.ejmech.2010.04.015. Epub 2010 Apr 18.
In the present study 18 novel imidazole-(benz)azole and imidazole-piperazine derivatives were synthesized in order to investigate their probable anticancer activity. The structures of the compounds were confirmed by IR, (1)H NMR and EI-MS spectral data. Cytotoxicity (MTT), analysis of DNA synthesis and detection of apoptotic DNA assays were applied to determine anticancer activity of the compounds against colon (HT-29) and breast (MCF-7) carcinoma cell lines. Most of the compounds, showed greater activity against HT-29 cells than MCF-7 cells. Some of them indicated considerable cytotoxicity against both of the carcinogenic cell lines. However, their inhibitory activity on DNA synthesis was relatively poor. Anticancer activity screening results revealed that 11, 12 and 13 were the most active compounds in the series. They exhibited significant cytotoxicity against both of the carcinogenic cell lines and caused DNA fragmentation of the HT-29 cells.
在本研究中，合成了 18 种新型咪唑-(苯)唑和咪唑-哌嗪衍生物，以研究它们可能的抗癌活性。通过红外光谱、(1)H NMR 和 EI-MS 光谱数据确认了化合物的结构。采用 MTT 法、DNA 合成分析和凋亡 DNA 检测法来测定化合物对结肠癌(HT-29)和乳腺癌(MCF-7)细胞系的抗癌活性。大多数化合物对 HT-29 细胞的活性大于 MCF-7 细胞。其中一些化合物对两种致癌细胞系表现出相当的细胞毒性。然而，它们对 DNA 合成的抑制活性相对较差。抗癌活性筛选结果表明，11、12 和 13 是该系列中最活跃的化合物。它们对两种致癌细胞系均表现出显著的细胞毒性，并导致 HT-29 细胞的 DNA 片段化。
