Marjanović Marko, Zorc Branka, Pejnović Lana, Zovko Marijana, Kralj Marijeta
Chem Biol Drug Des. 2007 Mar;69(3):222-6. doi: 10.1111/j.1747-0285.2007.00494.x.
Following numerous experimental observations that various non-steroidal anti-inflammatory drugs have antitumor potentials, a series of fenoprofenamides (1a-g) and ketoprofenamides (2a-c) was tested on proliferation of different human tumor cell lines and normal human fibroblasts in vitro. Fenoprofen and ketoprofen showed modest antiproliferative activity, whereas the growth inhibitory activity of the tested amides clearly demonstrates that the substituents linked by an amide bond are essential for the significantly stronger cytostatic activity, probably because of a greater lipophilicity and/or better cell uptake. Additionally, it was shown that the most active derivatives (1d and 2a) induced cell cycle arrest at the G1 phase, as well as apoptosis.
在众多实验观察表明各种非甾体抗炎药具有抗肿瘤潜力之后，对一系列苯氧苯丙酸酰胺（1a - g）和酮洛芬酰胺（2a - c）进行了体外不同人类肿瘤细胞系和正常人成纤维细胞增殖的测试。苯氧苯丙酸和酮洛芬显示出适度的抗增殖活性，而测试酰胺的生长抑制活性清楚地表明，通过酰胺键连接的取代基对于显著更强的细胞抑制活性至关重要，这可能是由于更大的亲脂性和/或更好的细胞摄取。此外，研究表明最具活性的衍生物（1d和2a）诱导细胞周期停滞在G1期以及凋亡。
