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Novel bis-ortho-alkoxy-para-piperazinesubstituted-2,4-dianilinopyrimidines (KRCA-0008) as potent and selective ALK inhibitors for anticancer treatment |
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| Authors: | 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 |
| Institution: | 1. Bio-Organic Science Division, Korea Research Institute of Chemical Technology, PO Box 107, Daejeon 305-600, Republic of Korea;2. Medicinal & Pharmaceutical Chemistry, University of Science & Technology, Daejeon 305-350, Republic of Korea;3. Korea Chemical Bank, Daejeon 305-600, Republic of Korea;4. College of Pharmacy, Chungbuk National University, Cheongju 361-763, Republic of Korea;5. College of Pharmacy, Chungnam National University, Daejeon 305-764, Republic of Korea |
| 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: | ALK ACK1 Kinases NSCLC Diaminopyrimidine Inhibitors |
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