AI Article Synopsis
- Researchers modified ciprofloxacin by replacing its C3 carboxyl group with a heterocyclic ring, creating new compounds known as cyclopropyl fluoroquinolone aminothiadiazole scaffolds.
- These new compounds were then reacted with aromatic aldehydes to produce Schiff bases (3a-3j), which were structurally analyzed and tested for their antitumor properties.
- The study found that eleven of these derivatives exhibited significant cytotoxicity against various cancer cell lines, indicating that the original carboxyl group in fluoroquinolone is not essential for antitumor effectiveness and suggesting that these modified fluoroquinolone compounds warrant further investigation.
Article Abstract
To discover a novel antitumor lead compound derived from fluoroquinolone, C3 carboxyl group of ciprofloxacin (1) was replaced with heterocyclic ring to form cyclopropyl fluoroquinolone aminothiadiazole scaffold (2), then reacted with aromatic aldehydes to give the Schiff bases compounds (3a-3j). The structures of new compounds were characterized by element analysis and spectral data, and their in vitro antitumor activity against SMMC-7721, HL60 and L1210 cell lines was evaluated by MTT assay via the respective IC50 values. The bioactive assay showed that eleven thiadiazole-substituted ciprofloxacin derivatives displayed potential cytotoxicity against the tested cancer cell lines, where the IC50 values of compounds 3d and 3f reached micromolar concentration. Therefore, the C3 carboxyl group of fluoroquinolone is not necessary to antitumor activity. Functionally modified heterocycle-substituted fluoroquinolone as potent antitumor lead compound is valuable for further study.
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