Synthesis and antitumor activity of C3 heterocyclic-substituted fluoroquinolone derivatives (I): ciprofloxacin aminothiodiazole Schiff-bases / 药学学报
Acta Pharmaceutica Sinica
;
(12): 1112-1115, 2008.
Article
Dans Chinois
| WPRIM
| ID: wpr-232634
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.
Texte intégral:
Disponible
Indice:
WPRIM (Pacifique occidental)
Sujet Principal:
Anatomopathologie
/
Pharmacologie
/
Bases de Schiff
/
Tests de criblage d'agents antitumoraux
/
Leucémie L1210
/
Ciprofloxacine
/
Cellules HL-60
/
Concentration inhibitrice 50
/
Lignée cellulaire tumorale
/
Tumeurs du foie
Limites du sujet:
Animaux
/
Humains
langue:
Chinois
Texte intégral:
Acta Pharmaceutica Sinica
Année:
2008
Type:
Article
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