Part IV: Design, synthesis and antitumor activity of fluoroquinolone C-3 heterocycles: bis-oxadiazole methylsulfide derivatives derived from ciprofloxacin / 药学学报
Acta Pharmaceutica Sinica
;
(12): 1017-1022, 2012.
Artículo
en Inglés
| WPRIM
| ID: wpr-276206
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).
Texto completo:
Disponible
Índice:
WPRIM (Pacífico Occidental)
Asunto principal:
Oxadiazoles
/
Farmacología
/
Piperazinas
/
Diseño de Fármacos
/
Estructura Molecular
/
Leucemia L1210
/
Ciprofloxacina
/
Química
/
Cricetulus
/
Células CHO
Límite:
Animales
/
Humanos
Idioma:
Inglés
Revista:
Acta Pharmaceutica Sinica
Año:
2012
Tipo del documento:
Artículo
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