期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 29, 期 12, 页码 1514-1517出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2019.04.012
关键词
Anaplastic lymphoma kinase; ALK; Non-small cell lung cancer; NSCLC; Kinase; Inhibitor; Ceritinib; Deuterated drug
Anaplastic lymphoma kinase (ALK) is an attractive therapeutic target for the treatment of non-small cell lung cancer (NSCLC). Within our ALK drug discovery program, we identified novel deuterated 2,4-diarylamino pyrimidine compounds as potent ALK inhibitors. The compound 11 showed better in vitro activity and in vivo efficacy with good pharmacokinetic profile. In vivo efficacy of compound 11 was better than standard drug ceritinib in NCI-H2228 xenograft mice model.
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