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| 標題: | Combretastatin A-4 derivatives: synthesis and evaluation of 2,4,5-triaryl-1H-imidazoles as potential agents against H1299 (non-small cell lung cancer cell) |
| 作者: | Tseng, Chih-Hua
Li, Chi-Yi
Chiu, Chien-Chih
Hu, Huei-Ting
Han, Chein-Hwa
Chen, Yeh-Long
Tzeng, Cherng-Chyi |
| 貢獻者: | 藥學系 |
| 關鍵字: | Combretastatin A-4 (Ca-4)
Triarylimidazoles
H1299
Cytotoxicity
Cell Cycle |
| 日期: | 2012-11 |
| 上傳時間: | 2014-03-21 16:12:42 (UTC+8) |
| 出版者: | Springer |
| 摘要: | A number of 2,4,5-triaryl-1H-imidazole derivatives were synthesized and evaluated for their antiproliferative activities against the growth of five cell lines including three non-small cell lung cancers (H460, H1299, and A549), one breast cancer (MCF-7), and one normal diploid embryonic lung cell line (MRC-5). Preliminary results indicated that both 2-(5-bromofuran-2-yl)-4,5-bis{4-[3-(dimethylamino) propoxy] phenyl}-1H-imidazole (10f) and 4,5-bis{4-[3-(dimethylamino)propoxy]phenyl}-2-(5-nitrofuran-2-yl)-1H -imidazole (10g) were selectively active against the growth of H1229 with an IC50 of less than 0.1 mu M, thus were more active than topotecan (IC50 > 10.0 mu M). However, both 10f and 10g exhibited only marginal cytotoxicity against H460, A549, MCF-7, and MRC-5 requiring an IC (50) of at least 4.16 mu M. Our results also indicated that 10f induced H1299 cell cycle arrest at G0/G1 through the inactivation of p38 MAPK, JNK, ERK, as well as the expression of SIRT1 and survivin. These results suggested that 10f might have therapeutic potential against H1299 (non-small cell lung cancer cell). |
| 關聯: | Molecular Diversity, 16(4), 697-709 |
| 顯示於類別: | [藥學系(所)] 期刊論文
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