Abstract
Five novel 8-nitrociprofloxacin-1,2,3-triazole conjugates(9a-e) were synthesized via 1,3-dipolar cycloaddition reaction, by reacting ethyl 1-cyclopropyl-6-fluoro-8-nitro-4-oxo-7-(4-(3-oxobutanoyl) piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylate(7) with various aryl azides. The new compounds were characterized using High-Resolution Mass Spectrometry(HRMS), 1H NMR, and 13C NMR. Conjugates(9a-e) were tested for their in vitro anticancer activity against two prostate cancer cell lines, namely, PC3, DU145. Conjugates 9d and 9e exhibited remarkable anti-proliferative activity against DU145 and PC3 cell-lines. The IC50 of 9d and 9e for PC3 cell line is 0.0496 ± 0.2372 μM and 0.145 ± 0.337 μM, respectively. All derivatives (9a-e) significantly increased the amount of DNA damage. Two conjugates 9d and 9e, showed enhanced cytotoxic activity against both prostate cancer cell lines in comparison to the other conjugates. Derivatives 9e, 9c and 9d significantly enhanced the expression of p53, Caspases3 and p21 by 4-folds. The AnnexinV–FITC/PI test revealed a late apoptosis at the level of 9.1–13.5 % as performed with DU145 cells cultured with derivatives 9e and 9d.
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