Novel bis-ortho-alkoxy-para-piperazinesubstituted-2,4-dianilinopyrimidines (KRCA-0008) as potent and selective ALK inhibitors for anticancer treatment
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- 作者：Chi Hoon Park ; Hyeonjeong Choe ; In-Young Jang ; So Yeong Kwon ; Muhammad Latif ; Heung Kyoung Lee ; Hyeon Ji Lee ; Eun Hye Yang ; Jeong In Yun ; Chong Hak Chae ; Sung Yun Cho ; Sang Un Choi ; Jae Du Ha ; Heejung Jung ; Hyoung Rae Kim ; Pilho Kim ; Chong Ock Lee ; Chang-Soo Yun ; Kwangho Lee
- 关键词：ALK ; ACK1 ; Kinases ; NSCLC ; Diaminopyrimidine ; Inhibitors ; N-Acetylpiperidine
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2013
- 出版时间：15 November, 2013
- 年：2013
- 卷：23
- 期：22
- 页码：6192-6196
- 全文大小：927 K
文摘
The synthesis of bis-ortho-alkoxy-para-piperazinesubstituted-2,4-dianilinopyrimidines is described and their structure-activity-relationship to anaplastic lymphoma kinase (ALK) is presented. KRCA-0008 is selective and potent to ALK and Ack1, and displays drug-like properties without hERG liability. KRCA-0008 demonstrates in vivo efficacy comparable to Crizotinib in xenograft mice model.