Researchers from Kaohsiung Medical University, Taiwan, have synthesised and tested a number of 2,3-diarylquinoline derivatives for anticancer activities, one of which showed significant potential preventing cell growth in certain cancer cell lines.
Cherng-Chyi Tzeng and colleagues synthesised the 2,3-diarylquinoline derivatives as part of a continuing study to explore potent anticancer drug candidates. The quinoline skeleton is prevalent in many natural and synthetic heterocycles with a wide range of biological effects, including antitumor activity. The structures of tamoxifen and combretastatin A-4, two potent anticancer agents, were modified to include the quinoline moiety and various side chains to improve their activity.
Testing against six cancer cell lines, including human hepatocelluar carcinoma, non-small cell lung cancer and breast cancer, revealed one compound that was more active than tamoxifen. 6-fluoro-2,3-bis{4-[2-(piperidin-1-yl)ethoxy]phenyl}quinoline-otherwise known in this paper as the more manageable 16b-was shown to induce cell cycle arrest at the G2/M phase, resulting ultimately in cell death in half of the tested cell lines. Work is ongoing to optimise the structure.
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Synthesis and antiproliferative evaluation of 2,3-diarylquinoline derivatives
Chih-Hua Tseng, Yeh-Long Chen, Kuin-Yu Chung, Chi-Huei Wang, Shin-I Peng, Chih-Mei Cheng and Cherng-Chyi Tzeng
Org. Biomol. Chem., 2011, Advance Article
DOI: 10.1039/C0OB01225D
