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Novel bis-ortho-alkoxy-para-piperazinesubstituted-2,4-dianilinopyrimidines (KRCA-0008) as potent and selective ALK inhibitors for anticancer treatment

2013; Elsevier BV; Volume: 23; Issue: 22 Linguagem: Inglês

10.1016/j.bmcl.2013.08.090

1464-3405

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, Kwang‐Ho Lee,

Synthesis and Biological Evaluation

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.