Literature DB >> 26235945

Synthesis and evaluation of novel 2,4-diaminopyrimidines bearing bicyclic aminobenzazepines for anaplastic lymphoma kinase (ALK) inhibitor.

Ga Ae Kang1, Minji Lee2, Dawn Song3, Heung Kyoung Lee1, Sunjoo Ahn4, Chi Hoon Park4, Chong Ock Lee1, Chang Soo Yun4, Heejung Jung4, Pilho Kim4, Jae Du Ha1, Sung Yun Cho4, Hyoung Rae Kim5, Jong Yeon Hwang6.   

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.
Copyright © 2015 Elsevier Ltd. All rights reserved.

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Keywords:  2,4-Diaminopyrimidine; ALK; Cancer

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Year:  2015        PMID： 26235945     DOI： 10.1016/j.bmcl.2015.07.004

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  1 in total

1.  Synthesis of a [(18)F]-labeled ceritinib analogue for positron emission tomography of anaplastic lymphoma kinase, a receptor tyrosine kinase, in lung cancer.

Authors:  Sandun Perera; David Piwnica-Worms; Mian M Alauddin
Journal:  J Labelled Comp Radiopharm       Date:  2016-02-08       Impact factor: 1.921
  1 in total

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