Design and synthesis of novel 3-sulfonylpyrazol-4-amino pyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors. Issue 8 (15th April 2016)

• Record Type: Journal Article
• Authors: Zhang, Peilong; Dong, Jiaqiang; Zhong, Boyu; Zhang, Deyi; Yuan, Hongbin; Jin, Can; Xu, Xiangyuan; Li, Hailong; Zhou, Yong; Liang, Zhi; Ji, Minghua; Xu, Tao; Song, Guowei; Zhang, Ling; Chen, Gang; Meng, Xuejing; Sun, Desheng; Shih, Joe; Zhang, Ruihao; Hou, Guojun; Wang, Chengcheng; Jin, Ying; Yang, Qiong
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 8(2016)
• Page Start: 1910
• Page End: 1918
• Publication Date: 2016-04-15
• Subjects: ALK -- Kinase -- Anti-tumor -- NSCLC -- Pyrimidine; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.03.017
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: Anaplastic 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 compound53 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.