Fenoprofen and ketoprofen amides as potential antitumor agents.
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.
Marjanović
Marko
M
Zorc
Branka
B
Pejnović
Lana
L
Zovko
Marijana
M
Kralj
Marijeta
M
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
D000577:Amides; D000970:Antineoplastic Agents; D007660:Ketoprofen; D005279:Fenoprofen