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

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

Bioorganic & Medicinal Chemistry Letters（2013）

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摘要

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.

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关键词

ALK,ACK1,Kinases,NSCLC,Diaminopyrimidine,Inhibitors,N-Acetylpiperidine

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