4区 · 医学
Article
作者: Jin, Can ; Meng, Xuejing ; Shih, Joe ; Dong, Jiaqiang ; Zhong, Boyu ; Li, Hailong ; Xu, Xiangyuan ; Ji, Minghua ; Sun, Desheng ; Chen, Gang ; Zhang, Ruihao ; Zhang, Peilong ; Zhang, Deyi ; Yang, Qiong ; Song, Guowei ; Jin, Ying ; Hou, Guojun ; Xu, Tao ; Zhang, Ling ; Liang, Zhi ; Zhou, Yong ; Wang, Chengcheng ; Yuan, Hongbin
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 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.