| Literature DB >> 24095090 |
Chi Hoon Park1, 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.
Abstract
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.Entities:
Keywords: ACK1; ALK; Diaminopyrimidine; Inhibitors; Kinases; N-Acetylpiperidine; NSCLC
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Year: 2013 PMID： 24095090 DOI： 10.1016/j.bmcl.2013.08.090
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823