Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase.

@article{Huang2016DiscoveryOB,
  title={Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase.},
  author={Wei-Sheng Huang and Shuangying Liu and Dong Zou and Mathew Thomas and Yihan Wang and Tianjun Zhou and Jan Romero and Anna Kohlmann and Feng Li and Jiwei Qi and Lisi Cai and Timothy A. Dwight and Yongjin Xu and Rongsong Xu and Rory Dodd and Angela Toms and Lois E Parillon and Xiaohui Lu and Rana Anjum and Sen Zhang and Frank Zhen Wang and Jeffrey A. Keats and Scott D. Wardwell and Yaoyu Ning and Qihong Xu and Lauren E Moran and Qurish K. Mohemmad and Hyun Gyung Jang and Tim Clackson and Narayana I. Narasimhan and V. Rivera and Xiaotian Zhu and David C Dalgarno and William Shakespeare},
  journal={Journal of medicinal chemistry},
  year={2016},
  volume={59 10},
  pages={4948-64}
}
In the treatment of echinoderm microtubule-associated protein-like 4 (EML4)-anaplastic lymphoma kinase positive (ALK+) non-small-cell lung cancer (NSCLC), secondary mutations within the ALK kinase domain have emerged as a major resistance mechanism to both first- and second-generation ALK inhibitors. This report describes the design and synthesis of a series of 2,4-diarylaminopyrimidine-based potent and selective ALK inhibitors culminating in identification of the investigational clinical… CONTINUE READING
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