Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, Cairo 11562, Egypt.
Eur J Med Chem. 2013 May;63:826-32. doi: 10.1016/j.ejmech.2013.03.008. Epub 2013 Mar 16.
Several derivatives with a quinoline scaffold and a flexible, semi-flexible or rigid side chains at position 8 of the quinoline ring were synthesized and assessed for their in vitro activity versus the human colon cancer cell line HT29 and the human breast cancer cell line MDA-MB231. The HT29 cell line was more refractory to the cytotoxic activity of some compounds, meanwhile all the quinoline derivatives except one displayed high to moderate activity against MDA-MB231 with IC50 values ranging between 4.6 and 48.2 μM. The most active derivative in this study against both tested cell lines was the Schiff's base 4e with IC50 of 4.7 and 4.6 μM against HT29 and MDA-MB231, respectively.
合成了几个具有喹啉骨架的衍生物,并在喹啉环的 8 位上带有柔性、半柔性或刚性侧链,评估了它们对人结肠癌细胞系 HT29 和人乳腺癌细胞系 MDA-MB231 的体外活性。HT29 细胞系对一些化合物的细胞毒性活性更具抗性,同时除一个化合物外,所有喹啉衍生物对 MDA-MB231 均表现出高至中度的活性,IC50 值在 4.6 至 48.2 μM 之间。在这项研究中,对两种测试细胞系最具活性的衍生物是席夫碱 4e,对 HT29 和 MDA-MB231 的 IC50 值分别为 4.7 和 4.6 μM。