Synthesis and antiproliferative activity of 1-[(sub)]-6-fluoro-3-[(sub)]-1, 3,4-oxadiazol-2-yl-7-piperazino-1, 4-dihydro-4-quinolinone derivatives

A series of 1-(sub)]-6-fluoro-3- (sub)]-1, 3, 4-oxadiazol-2-yl-7-piperazino-1, 4-dihydro 4-quinolinones were synthesized by the reaction between ciprofloxacin and norfloxacin with an appropriate acid hydrazide in phosphorous oxychloride. All newly synthesized compounds were evaluated for their antiproliferative activities against human lung tumor cell lines (A 549). Fluoroquinolone with oxadiazole (Q ₂ ) 1-cyclopropyl-6-fluoro-3- 5-(4-nitrophenyl)-1,3,4-oxadiazol-2-yl]-7-piperazino-1, 4-dihydro-4-quinolinone was found to be the most active compound in vitro with a half-maximal inhibitory concentration (IC₅₀) of 9.0 μg/mL.