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

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, …
Bioorganic & medicinal chemistry letters, Vol.23(22), pp.6192-6196
15/11/2013
DOI: https://doi.org/10.1016/j.bmcl.2013.08.090
PMID: 24095090

Abstract

ACK1 ALK Diaminopyrimidine Inhibitors Kinases N-Acetylpiperidine NSCLC
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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