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

…, EH Yang, JI Yun, CH Chae, SY Cho, SU Choi…

Index: Park, Chi Hoon; Choe, Hyeonjeong; Jang, In-Young; Kwon, So Yeong; Latif, Muhammad; Lee, Heung Kyoung; Lee, Hyeon Ji; Yang, Eun Hye; Yun, Jeong In; Chae, Chong Hak; Cho, Sung Yun; Choi, Sang Un; Ha, Jae Du; Jung, Heejung; Kim, Hyoung Rae; Kim, Pilho; Lee, Chong Ock; Yun, Chang-Soo; Lee, Kwangho Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 22 p. 6192 - 6196

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Citation Number: 10

Abstract

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.