Synthesis and antitumor activity of novel 2-(1-substituted-piperidin-4-ylamino)quinazolines as antitumor agents.
- Author:
Yong-Kang WANG
1
;
Jing JIN
;
Li-Na ZHU
;
Yi ZHANG
;
Xiao-Guang CHEN
;
Xin-Qin GAO
;
Bai-Ling XU
Author Information
1. Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China. .
- Publication Type:Journal Article
- MeSH:
Animals;
Antineoplastic Agents;
chemical synthesis;
chemistry;
pharmacology;
Carcinoma, Lewis Lung;
pathology;
Cell Line, Tumor;
Drug Screening Assays, Antitumor;
Inhibitory Concentration 50;
Liver Neoplasms;
pathology;
Male;
Mice;
Mice, Inbred C57BL;
Neoplasm Transplantation;
Quinazolines;
chemical synthesis;
chemistry;
pharmacology
- From:
Acta Pharmaceutica Sinica
2012;47(9):1164-1178
- CountryChina
- Language:English
-
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).
