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Synthesis and evaluation of novel 2,4-diaminopyrimidines bearing bicyclic aminobenzazepines for anaplastic lymphoma kinase (ALK) inhibitor.
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.
Afiliação
  • Kang GA; Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 305-600, Republic of Korea.
  • Lee M; Department of Chemistry, Korea University, Seoul 136-701, Republic of Korea.
  • Song D; College of Pharmacy, Chungbuk National University, Cheongju, Chungbuk 362-763, Republic of Korea.
  • Lee HK; Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 305-600, Republic of Korea.
  • Ahn S; Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 305-600, Republic of Korea; Department of Medicinal Chemistry and Pharmacology, University of Science & Technology, Daejeon 305-550, Republic of Korea.
  • Park CH; Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 305-600, Republic of Korea; Department of Medicinal Chemistry and Pharmacology, University of Science & Technology, Daejeon 305-550, Republic of Korea.
  • Lee CO; Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 305-600, Republic of Korea.
  • Yun CS; Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 305-600, Republic of Korea; Department of Medicinal Chemistry and Pharmacology, University of Science & Technology, Daejeon 305-550, Republic of Korea.
  • Jung H; Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 305-600, Republic of Korea; Department of Medicinal Chemistry and Pharmacology, University of Science & Technology, Daejeon 305-550, Republic of Korea.
  • Kim P; Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 305-600, Republic of Korea; Department of Medicinal Chemistry and Pharmacology, University of Science & Technology, Daejeon 305-550, Republic of Korea.
  • Ha JD; Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 305-600, Republic of Korea.
  • Cho SY; Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 305-600, Republic of Korea; Department of Medicinal Chemistry and Pharmacology, University of Science & Technology, Daejeon 305-550, Republic of Korea.
  • Kim HR; Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 305-600, Republic of Korea. Electronic address: hyngrk@krict.re.kr.
  • Hwang JY; Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 305-600, Republic of Korea; Department of Medicinal Chemistry and Pharmacology, University of Science & Technology, Daejeon 305-550, Republic of Korea. Electronic address: jyhwang@krict.re.kr.
Bioorg Med Chem Lett ; 25(18): 3992-8, 2015 Sep 15.
Article em En | MEDLINE | ID: mdl-26235945
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.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirimidinas / Benzazepinas / Compostos Bicíclicos com Pontes / Receptores Proteína Tirosina Quinases / Inibidores de Proteínas Quinases / Neoplasias Experimentais / Antineoplásicos Limite: Animals / Humans Idioma: En Ano de publicação: 2015 Tipo de documento: Article
Texto completo
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirimidinas / Benzazepinas / Compostos Bicíclicos com Pontes / Receptores Proteína Tirosina Quinases / Inibidores de Proteínas Quinases / Neoplasias Experimentais / Antineoplásicos Limite: Animals / Humans Idioma: En Ano de publicação: 2015 Tipo de documento: Article