Download MendeleyDesign and synthesis of novel 3-sulfonylpyrazol-4-amino pyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors.
Zhang, P., Dong, J., Zhong, B., Zhang, D., Yuan, H., Jin, C., Xu, X., Li, H., Zhou, Y., Liang, Z., Ji, M., Xu, T., Song, G., Zhang, L., Chen, G., Meng, X., Sun, D., Shih, J., Zhang, R., Hou, G., Wang, C., Jin, Y., Yang, Q.(2016) Bioorg Med Chem Lett 26: 1910-1918
- PubMed: 26979157
- DOI: https://doi.org/10.1016/j.bmcl.2016.03.017
- Primary Citation of Related Structures:
5IMX - PubMed 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 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.
Organizational Affiliation:
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.
