AI Article Synopsis
- - The study focuses on enhancing anticancer properties of fluoroquinolone candidates derived from ciprofloxacin by modifying a specific chemical structure (C3 carboxyl group).
- - A crucial intermediate, oxadiazole thiol, was synthesized and further transformed into bis-oxadiazole methylsulfides and dimethylpiperazinium iodides.
- - Initial testing indicates that the piperazinium compounds demonstrate stronger anticancer effectiveness in vitro against various cancer cell lines compared to their free base counterparts.
Article Abstract
To explore an efficient strategy for further development of anticancer fluoroquinolone candidates derived from ciprofloxacin, a heterocyclic ring as the bioisosteric replacement of C3 carboxyl group led to a key intermediate, oxadiazole thiol (5), which was further modified to the bis-oxadiazole methylsulfides (7a-7h) and the corresponding dimethylpiperazinium iodides (8a-8h), respectively. Structures were characterized by elemental analysis and spectra data, and their anticancer activities in vitro against CHO, HL60 and L1210 cancer cells were also evaluated by MTT assay. The preliminary results show that piperazinium compounds (8) possess more potent activity than that of corresponding free bases (7).
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