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Acta Pharmaceutica Sinica ; (12): 1164-1178, 2012.
Artículo en Inglés | WPRIM | ID: wpr-274682

RESUMEN

A variety of novel 2-(1-substituted-piperidine-4-ylamino)quinazoline derivatives were prepared and their antiproliferative activities on five cancer cell lines were evaluated by MTT assay. Quinazolines 4j-4l, 5a, 5b and 5d bearing a small hydrophobic alkyl group on piperidine ring exhibited potent antitumor activities with IC50 values at micromolar level. Compound 41 displayed significant in vivo antitumor activity with 72.9% inhibition on H22 tumor growth and 80% inhibition on Lewis lung cancer growth at a dose of 200 mg x kg(-1).


Asunto(s)
Animales , Masculino , Ratones , Antineoplásicos , Química , Farmacología , Carcinoma Pulmonar de Lewis , Patología , Línea Celular Tumoral , Ensayos de Selección de Medicamentos Antitumorales , Concentración 50 Inhibidora , Neoplasias Hepáticas , Patología , Ratones Endogámicos C57BL , Trasplante de Neoplasias , Quinazolinas , Química , Farmacología
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