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Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor.
Yu, Tao; Zhang, Yonglian; Kerekes, Angela D; Tagat, Jayaram R; Doll, Ronald J; Xiao, Yushi; Esposite, Sara; Hruza, Alan; Belanger, David B; Voss, Matthew; Rainka, Matthew P; Basso, Andrea; Liu, Ming; Liang, Lianzhu; Sui, Ning; Prelusky, Daniel; Rindgen, Diane; Zhang, Likang.
Affiliation
  • Yu T; Department of Chemical Research, MRL 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. Electronic address: tao.yu@merck.com.
  • Zhang Y; Department of Chemical Research, MRL 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Kerekes AD; Department of Chemical Research, MRL 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Tagat JR; Department of Chemical Research, MRL 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Doll RJ; Department of Chemical Research, MRL 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Xiao Y; Department of Chemical Research, MRL 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Esposite S; Department of Chemical Research, MRL 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Hruza A; Department of Structural Chemistry, MRL 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Belanger DB; Department of Chemical Research, MRL 320 Bent Street, Cambridge, MA 02141, USA.
  • Voss M; AMRI, 26 Corporate Circle, PO Box 15098, Albany, NY 12212, USA.
  • Rainka MP; AMRI, 26 Corporate Circle, PO Box 15098, Albany, NY 12212, USA.
  • Basso A; Department of Oncology, MRL 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Liu M; Department of Oncology, MRL 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Liang L; Department of Oncology, MRL 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Sui N; Department of Oncology, MRL 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Prelusky D; Department of DMPK, MRL 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Rindgen D; Department of DMPK, MRL 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Zhang L; Department of Chemical Research, MRL 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
Bioorg Med Chem Lett ; 28(8): 1397-1403, 2018 05 01.
Article in En | MEDLINE | ID: mdl-29545102
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyrazines / Protein Kinase Inhibitors / Aurora Kinase A / Aurora Kinase B / Imidazoles / Antineoplastic Agents Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2018 Document type: Article Country of publication: Reino Unido
Fulltext
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyrazines / Protein Kinase Inhibitors / Aurora Kinase A / Aurora Kinase B / Imidazoles / Antineoplastic Agents Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2018 Document type: Article Country of publication: Reino Unido