Synthesis and evaluation of novel 2, 4-diaminopyrimidines bearing bicyclic aminobenzazepines for anaplastic lymphoma kinase (ALK) inhibitor. Issue 18 (15th September 2015)

• Record Type: Journal Article
• Authors: Kang, Ga Ae; Lee, Minji; Song, Dawn; Lee, Heung Kyoung; Ahn, Sunjoo; Park, Chi Hoon; Lee, Chong Ock; Yun, Chang Soo; Jung, Heejung; Kim, Pilho; Ha, Jae Du; Cho, Sung Yun; Kim, Hyoung Rae; Hwang, Jong Yeon
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 25:Issue 18(2015)
• Page Start: 3992
• Page End: 3998
• Publication Date: 2015-09-15
• Subjects: Cancer -- ALK -- 2, 4-Diaminopyrimidine; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.07.004
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: A 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.