新型3-磺酰基吡唑-4-氨基嘧啶作为强效间变性淋巴瘤激酶（ALK）抑制剂的设计与合成
Design and synthesis of novel 3-sulfonylpyrazol-4-amino pyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors.
作者信息
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
机构信息
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.
Crown Bioscience Inc. (Taicang), 6 Beijing West Road, Taicang Economic Development Area, Taicang 215400, China.
出版信息
Bioorg Med Chem Lett. 2016 Apr 15;26(8):1910-8. doi: 10.1016/j.bmcl.2016.03.017. Epub 2016 Mar 7.
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.
间变性淋巴瘤激酶（ALK）是治疗某些非小细胞肺癌患者极具吸引力的治疗靶点。本信函描述了对新型3-磺酰基吡唑-4-氨基嘧啶骨架的进一步构效关系研究。这项工作确定了一种化合物53，它具有非常好的体外/体内疗效、良好的药物代谢动力学性质以及更好的人乙醚相关基因（hERG）耐受性，目前正在进行分析评估，以作为潜在的临床前候选药物。
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