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

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

  • Bioorg Med Chem Lett. 2013 Nov 15;23(22):6192-6. doi: 10.1016/j.bmcl.2013.08.090.
Chi Hoon Park 1,  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
Affiliations

Affiliation

  • 1 Bio-Organic Science Division, Korea Research Institute of Chemical Technology, PO Box 107, Daejeon 305-600, Republic of Korea.
PMID: 24095090 DOI: 10.1016/j.bmcl.2013.08.090
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.

Keywords

ACK1; ALK; Diaminopyrimidine; Inhibitors; Kinases; N-Acetylpiperidine; NSCLC.

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