Synthesis and potential antitumor activity of 7-(4-substituted piperazin-1-yl)-4-oxoquinolines based on ciprofloxacin and norfloxacin scaffolds: in silico studies.

摘要: The potential antitumor activities of a series 7-(4-substituted piperazin-1-yl)fluoroquinolone derivatives (1-14a,b) using ciprofloxacin and norfloxacin as scaffolds are described. These compounds exhibit potent broad spectrum 60 human cell lines in addition to the inherent antibacterial activity. Compounds 1a, 2a, 3b, 6b 7a were found be most potent, while 2b, 5b, 6a have an average results this study demonstrated that (mean GI50; 2.63-3.09 µM) nearly 7-fold more compared with positive control 5-fluorouracil 22.60 µM). More interestingly, almost activity similar gefitinib 3.24 µM) 2-fold erlotinib 7.29 µM). In silico ADME-Tox prediction methodology used active identify structural features required for