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.
Todd Groessl合作论文数3Jie Li合作论文数3
Tove Tuntland合作论文数3Auzon Steffy合作论文数2Yelena Sarkisova合作论文数2Wenshuo Lu合作论文数2You-Qun He合作论文数2Wendy Richmond合作论文数2Christian Lee合作论文数2Sungjoon Kim合作论文数2Nanxin Li合作论文数2Jin Yunho合作论文数2Phimister Andrew合作论文数2Kim Young合作论文数2Chen Bei合作论文数2Pei Wei合作论文数2
Tao Jiang (蒋涛)合作论文数Department of Electronic and Information Engineering, Huazhong University of Science and Technology, Wuhan 430074, China
College of Computer Science and Technology, Huazhong University of Science and Technology, Wuhan, China 430074 and Department of Computer Science, Hengyang Normal University, Hengyang, China 421008
Shanghai Globalization Laboratory, IBM, China2Badry Bursulaya合作论文数2
Sean B. Joseph合作论文数2Tetsuo Uno合作论文数2Pierre-Yves Michellys合作论文数2Thomas H. Marsilje合作论文数2Bo Liu合作论文数2Jonathan Chang合作论文数2Jennifer L Harris合作论文数1Celin Tompkins合作论文数1Greg Chopiuk合作论文数1Ruo Steensma合作论文数1John Isbell合作论文数1Mei-Ting Vaillancourt合作论文数1Jennifer Harris合作论文数1Michael Shapiro合作论文数1J Alex Aycinena合作论文数1M. Warmuth合作论文数1Yongqin Wan合作论文数1jiqing jiang合作论文数1Kevin Johnson合作论文数1
X. Allen Li合作论文数Department of Radiation Oncology, Medical College of Wisconsin1Lelais Gerald合作论文数1Sun Frank合作论文数1Li Chun合作论文数1Pferdekamper AnneMarie C合作论文数1Jia Yong合作论文数1
Nathanael S. Gray合作论文数Stanford University;Dana-Farber Cancer Institute;Harvard Medical School1Donald S. Karanewsky合作论文数1H. Martin Seidel合作论文数1Shailaja Kasibhatla合作论文数1Perry Gordon合作论文数1
