Synthesis and evaluation of novel 2,4-diaminopyrimidines bearing bicyclic aminobenzazepines for anaplastic lymphoma kinase (ALK) inhibitor
2015; Elsevier BV; Volume: 25; Issue: 18 Linguagem: Inglês
10.1016/j.bmcl.2015.07.004
ISSN1464-3405
AutoresGa Ae Kang, Minji Lee, Dawn Song, Heung Kyoung Lee, Sunjoo Ahn, Chi Hoon Park, Chong Ock Lee, Chang Soo Yun, Heejung Jung, Pilho Kim, Jae Du Ha, Sung Yun Cho, Hyoung Rae Kim, Jong Yeon Hwang,
Tópico(s)Synthesis and Biological Evaluation
ResumoA series of novel 2,4-diaminopyrimidine compounds bearing bicyclic aminobenzazepine were synthesized and evaluated for their anti-ALK activities. The activities of these compounds were confirmed in both enzyme- and cell-based ALK assays. Amongst compounds synthesized, KRCA-0445 showed very promising results in pharmacokinetic study and in vivo efficacy study with H3122 xenograft mouse model.
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