title: Fenoprofen and ketoprofen amides as potential antitumor agents.
abstract: 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.
authors: Marko
authors: M
authors: Marjanović
authors: Branka
authors: B
authors: Zorc
authors: Lana
authors: L
authors: Pejnović
authors: Marijana
authors: M
authors: Zovko
authors: Marijeta
authors: M
authors: Kralj
mesh_terms: D000577:Amides / Q000737:chemistry*; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D005279:Fenoprofen / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D007660:Ketoprofen / Q000737:chemistry* / Q000494:pharmacology*; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D000970:Antineoplastic Agents; D007660:Ketoprofen; D005279:Fenoprofen