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Bioorg. Med. Chem. Lett. · Apr 2016
Design and synthesis of novel 3-sulfonylpyrazol-4-amino pyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors.
- Peilong Zhang, Jiaqiang Dong, Boyu Zhong, Deyi Zhang, Hongbin Yuan, Can Jin, Xiangyuan Xu, Hailong Li, Yong Zhou, Zhi Liang, Minghua Ji, Tao Xu, Guowei Song, Ling Zhang, Gang Chen, Xuejing Meng, Desheng Sun, Joe Shih, Ruihao Zhang, Guojun Hou, Chengcheng Wang, Ying Jin, and Qiong Yang.
- Department of Applied Chemistry, Beijing Institute of Technology, Zhongguancun South Street, Beijing 100081, China; Beijing Pearl Biotech Ltd, No. 203, Section 2, Wangjing Lize Zhongyuan, Chaoyang District, Beijing 100102, China.
- Bioorg. Med. Chem. Lett. 2016 Apr 15; 26 (8): 1910-8.
AbstractAnaplastic lymphoma kinase (ALK) is a highly attractive therapeutic target for the treatment of some non-small cell lung cancer patients. This Letter describes the further SAR exploration on the novel 3-sulfonylpyrazol-4-amino pyrimidine scaffold. This work identified a compound 53 with very good in vitro/in vivo efficacies, good DMPK properties together with better hERG tolerability and it is currently being profiled for the evaluation as a potential pre-clinical candidate. Copyright © 2016 Elsevier Ltd. All rights reserved.
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