期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 56, 期 14, 页码 5675-5690出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm400402q
关键词
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The synthesis, preclinical profile, and in vivo efficacy in rat xenograft models of the novel and selective anaplastic lymphoma kinase inhibitor 15b (LDK378) are described. In this initial report, preliminary structure-activity relationships (SARs) are described as well as the rational design strategy employed to overcome the development deficiencies of the first generation ALK inhibitor 4 (TAE684). Compound 15b is currently in phase 1 and phase 2 clinical trials with substantial antitumor activity being observed in ALK-positive cancer patients.
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