Synthesis and antitumor activity of novel 2-(1-substituted-piperidin-4-ylamino)quinazolines as antitumor agents / 药学学报
Acta Pharmaceutica Sinica
;
(12): 1164-1178, 2012.
Article
in English
| WPRIM
| ID: wpr-274682
ABSTRACT
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).
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pathology
/
Pharmacology
/
Quinazolines
/
Drug Screening Assays, Antitumor
/
Chemistry
/
Carcinoma, Lewis Lung
/
Inhibitory Concentration 50
/
Cell Line, Tumor
/
Liver Neoplasms
/
Mice, Inbred C57BL
Limits:
Animals
Language:
English
Journal:
Acta Pharmaceutica Sinica
Year:
2012
Type:
Article
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