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Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors.
Kettle, Jason G; Anjum, Rana; Barry, Evan; Bhavsar, Deepa; Brown, Crystal; Boyd, Scott; Campbell, Andrew; Goldberg, Kristin; Grondine, Michael; Guichard, Sylvie; Hardy, Christopher J; Hunt, Tom; Jones, Rhys D O; Li, Xiuwei; Moleva, Olga; Ogg, Derek; Overman, Ross C; Packer, Martin J; Pearson, Stuart; Schimpl, Marianne; Shao, Wenlin; Smith, Aaron; Smith, James M; Stead, Darren; Stokes, Steve; Tucker, Michael; Ye, Yang.
Afiliação
  • Kettle JG; Oncology, IMED Biotech Unit , AstraZeneca , Unit 310, Darwin Building, Cambridge Science Park, Milton Road , Cambridge CB4 0WG , United Kingdom.
  • Anjum R; Oncology, IMED Biotech Unit , AstraZeneca , 35 Gatehouse Park , Waltham , Massachusetts 02451 , United States.
  • Barry E; Oncology, IMED Biotech Unit , AstraZeneca , 35 Gatehouse Park , Waltham , Massachusetts 02451 , United States.
  • Bhavsar D; Oncology, IMED Biotech Unit , AstraZeneca , 35 Gatehouse Park , Waltham , Massachusetts 02451 , United States.
  • Brown C; Oncology, IMED Biotech Unit , AstraZeneca , 35 Gatehouse Park , Waltham , Massachusetts 02451 , United States.
  • Boyd S; Oncology, IMED Biotech Unit , AstraZeneca , Unit 310, Darwin Building, Cambridge Science Park, Milton Road , Cambridge CB4 0WG , United Kingdom.
  • Campbell A; Oncology, IMED Biotech Unit , AstraZeneca , Unit 310, Darwin Building, Cambridge Science Park, Milton Road , Cambridge CB4 0WG , United Kingdom.
  • Goldberg K; Oncology, IMED Biotech Unit , AstraZeneca , Unit 310, Darwin Building, Cambridge Science Park, Milton Road , Cambridge CB4 0WG , United Kingdom.
  • Grondine M; Oncology, IMED Biotech Unit , AstraZeneca , 35 Gatehouse Park , Waltham , Massachusetts 02451 , United States.
  • Guichard S; Oncology, IMED Biotech Unit , AstraZeneca , 35 Gatehouse Park , Waltham , Massachusetts 02451 , United States.
  • Hardy CJ; Discovery Sciences, IMED Biotech Unit , AstraZeneca , Unit 310, Darwin Building, Cambridge Science Park, Milton Road , Cambridge CB4 0WG , United Kingdom.
  • Hunt T; Oncology, IMED Biotech Unit , AstraZeneca , Unit 310, Darwin Building, Cambridge Science Park, Milton Road , Cambridge CB4 0WG , United Kingdom.
  • Jones RDO; Oncology, IMED Biotech Unit , AstraZeneca , Unit 310, Darwin Building, Cambridge Science Park, Milton Road , Cambridge CB4 0WG , United Kingdom.
  • Li X; Pharmaron Beijing Co., Ltd. , 6 Taihe Road BDA , Beijing 100176 , P. R. China.
  • Moleva O; Oncology, IMED Biotech Unit , AstraZeneca , Unit 310, Darwin Building, Cambridge Science Park, Milton Road , Cambridge CB4 0WG , United Kingdom.
  • Ogg D; Discovery Sciences, IMED Biotech Unit , AstraZeneca , Unit 310, Darwin Building, Cambridge Science Park, Milton Road , Cambridge CB4 0WG , United Kingdom.
  • Overman RC; Discovery Sciences, IMED Biotech Unit , AstraZeneca , Unit 310, Darwin Building, Cambridge Science Park, Milton Road , Cambridge CB4 0WG , United Kingdom.
  • Packer MJ; Oncology, IMED Biotech Unit , AstraZeneca , Unit 310, Darwin Building, Cambridge Science Park, Milton Road , Cambridge CB4 0WG , United Kingdom.
  • Pearson S; Oncology, IMED Biotech Unit , AstraZeneca , Unit 310, Darwin Building, Cambridge Science Park, Milton Road , Cambridge CB4 0WG , United Kingdom.
  • Schimpl M; Discovery Sciences, IMED Biotech Unit , AstraZeneca , Unit 310, Darwin Building, Cambridge Science Park, Milton Road , Cambridge CB4 0WG , United Kingdom.
  • Shao W; Oncology, IMED Biotech Unit , AstraZeneca , 35 Gatehouse Park , Waltham , Massachusetts 02451 , United States.
  • Smith A; Oncology, IMED Biotech Unit , AstraZeneca , Unit 310, Darwin Building, Cambridge Science Park, Milton Road , Cambridge CB4 0WG , United Kingdom.
  • Smith JM; Oncology, IMED Biotech Unit , AstraZeneca , Unit 310, Darwin Building, Cambridge Science Park, Milton Road , Cambridge CB4 0WG , United Kingdom.
  • Stead D; Oncology, IMED Biotech Unit , AstraZeneca , Unit 310, Darwin Building, Cambridge Science Park, Milton Road , Cambridge CB4 0WG , United Kingdom.
  • Stokes S; Oncology, IMED Biotech Unit , AstraZeneca , Unit 310, Darwin Building, Cambridge Science Park, Milton Road , Cambridge CB4 0WG , United Kingdom.
  • Tucker M; Oncology, IMED Biotech Unit , AstraZeneca , Unit 310, Darwin Building, Cambridge Science Park, Milton Road , Cambridge CB4 0WG , United Kingdom.
  • Ye Y; Pharmaron Beijing Co., Ltd. , 6 Taihe Road BDA , Beijing 100176 , P. R. China.
J Med Chem ; 61(19): 8797-8810, 2018 10 11.
Article em En | MEDLINE | ID: mdl-30204441

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Quinazolinas / Triazóis / Proteínas Proto-Oncogênicas c-kit / Tumores do Estroma Gastrointestinal / Inibidores de Proteínas Quinases / Proteínas Mutantes / Descoberta de Drogas / Mutação Tipo de estudo: Prognostic_studies Limite: Humans Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2018 Tipo de documento: Article País de afiliação: Reino Unido

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Quinazolinas / Triazóis / Proteínas Proto-Oncogênicas c-kit / Tumores do Estroma Gastrointestinal / Inibidores de Proteínas Quinases / Proteínas Mutantes / Descoberta de Drogas / Mutação Tipo de estudo: Prognostic_studies Limite: Humans Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2018 Tipo de documento: Article País de afiliação: Reino Unido