Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2

@article{Marsilje2013SynthesisSR,
  title={Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2},
  author={Thomas H. Marsilje and Wei Pei and Bei Chuan Chen and Wenshuo Lu and Tetsuo Uno and Yunho Jin and Tao Jiang and Sungjoon Kim and Nanxin Li and Markus Warmuth and Yelena Sarkisova and Frank Sun and Auzon Steffy and AnneMarie Culazzo Pferdekamper and Allen Guanqun Li and Sean B Joseph and Young -Hoon Kim and Bo Liu and Tove Tuntland and Xiaoming Cui and Nathanael S Gray and Ruo W Steensma and Yongqin Wan and Jiqing Jiang and Greg Chopiuk and J. Q. Li and William Perry Gordon and Wendy Richmond and Kevin M. Johnson and Jonathan Chang and Todd Groessl and You-Qun He and Andrew Phimister and Alex Aycinena and Christian C Lee and Badry D. Bursulaya and Donald S Karanewsky and H. Martin Seidel and Jennifer L. Harris and P Y Michellys},
  journal={Journal of medicinal chemistry},
  year={2013},
  volume={56 14},
  pages={5675-90}
}
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… CONTINUE READING
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