Design and synthesis of novel 3-sulfonylpyrazol-4-amino pyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors

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• 作者：Peilong Zhang^a ; ^c ; Jiaqiang Dong^b ; ^{djiaqiang@163.com" class="auth_mail" title="E-mail the corresponding author} ; Boyu Zhong^b ; Deyi Zhang^b ; Hongbin Yuan^b ; Can Jin^b ; Xiangyuan Xu^b ; Hailong Li^b ; Yong Zhou^b ; Zhi Liang^b ; Minghua Ji^b ; Tao Xu^b ; Guowei Song^b ; Ling Zhang^b ; Gang Chen^b ; Xuejing Meng^b ; Desheng Sun^b ; Joe Shih^b ; Ruihao Zhang^b ; Guojun Hou^b ; Chengcheng Wang^b ; Ying Jin^b ; Qiong Yang^b
• 关键词：ALK ; Kinase ; Anti-tumor ; NSCLC ; Pyrimidine
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：15 April 2016
• 年：2016
• 卷：26
• 期：8
• 页码：1910-1918
• 全文大小：3632 K

文摘

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.