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Discovery of a Thiadiazole-Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models.
Finlay, M Raymond V; Anderton, Mark; Bailey, Andrew; Boyd, Scott; Brookfield, Joanna; Cairnduff, Ceri; Charles, Mark; Cheasty, Anne; Critchlow, Susan E; Culshaw, Janet; Ekwuru, Tennyson; Hollingsworth, Ian; Jones, Neil; Leroux, Fred; Littleson, Mairi; McCarron, Hollie; McKelvie, Jennifer; Mooney, Lorraine; Nissink, J Willem M; Perkins, David; Powell, Steve; Quesada, Mar Jimenez; Raubo, Piotr; Sabin, Verity; Smith, James; Smith, Peter D; Stark, Andrew; Ting, Attilla; Wang, Peng; Wilson, Zena; Winter-Holt, Jon J; Wood, J Matthew; Wrigley, Gail L; Yu, Guoqing; Zhang, Peng.
Affiliation
  • Finlay MRV; Oncology, IMED Biotech Unit , AstraZeneca , 310, Cambridge Science Park, Milton Road , Cambridge CB4 0FZ , United Kingdom.
  • Anderton M; Oncology, IMED Biotech Unit , AstraZeneca , 310, Cambridge Science Park, Milton Road , Cambridge CB4 0FZ , United Kingdom.
  • Bailey A; Oncology, IMED Biotech Unit , AstraZeneca , 310, Cambridge Science Park, Milton Road , Cambridge CB4 0FZ , United Kingdom.
  • Boyd S; Oncology, IMED Biotech Unit , AstraZeneca , 310, Cambridge Science Park, Milton Road , Cambridge CB4 0FZ , United Kingdom.
  • Brookfield J; Cancer Research UK, Therapeutic Discovery Laboratories , Jonas Webb Building, Babraham Research Campus , Cambridge CB22 3AT , United Kingdom.
  • Cairnduff C; Cancer Research UK, Therapeutic Discovery Laboratories , Jonas Webb Building, Babraham Research Campus , Cambridge CB22 3AT , United Kingdom.
  • Charles M; Cancer Research UK, Therapeutic Discovery Laboratories , Jonas Webb Building, Babraham Research Campus , Cambridge CB22 3AT , United Kingdom.
  • Cheasty A; Cancer Research UK, Therapeutic Discovery Laboratories , Jonas Webb Building, Babraham Research Campus , Cambridge CB22 3AT , United Kingdom.
  • Critchlow SE; Oncology, IMED Biotech Unit , AstraZeneca , 310, Cambridge Science Park, Milton Road , Cambridge CB4 0FZ , United Kingdom.
  • Culshaw J; Oncology, IMED Biotech Unit , AstraZeneca , 310, Cambridge Science Park, Milton Road , Cambridge CB4 0FZ , United Kingdom.
  • Ekwuru T; Cancer Research UK, Therapeutic Discovery Laboratories , Jonas Webb Building, Babraham Research Campus , Cambridge CB22 3AT , United Kingdom.
  • Hollingsworth I; Oncology, IMED Biotech Unit , AstraZeneca , 310, Cambridge Science Park, Milton Road , Cambridge CB4 0FZ , United Kingdom.
  • Jones N; Cancer Research UK, Therapeutic Discovery Laboratories , Jonas Webb Building, Babraham Research Campus , Cambridge CB22 3AT , United Kingdom.
  • Leroux F; Cancer Research UK, Therapeutic Discovery Laboratories , Jonas Webb Building, Babraham Research Campus , Cambridge CB22 3AT , United Kingdom.
  • Littleson M; Oncology, IMED Biotech Unit , AstraZeneca , 310, Cambridge Science Park, Milton Road , Cambridge CB4 0FZ , United Kingdom.
  • McCarron H; Cancer Research UK, Therapeutic Discovery Laboratories , Jonas Webb Building, Babraham Research Campus , Cambridge CB22 3AT , United Kingdom.
  • McKelvie J; Cancer Research UK, Therapeutic Discovery Laboratories , Jonas Webb Building, Babraham Research Campus , Cambridge CB22 3AT , United Kingdom.
  • Mooney L; Oncology, IMED Biotech Unit , AstraZeneca , 310, Cambridge Science Park, Milton Road , Cambridge CB4 0FZ , United Kingdom.
  • Nissink JWM; Oncology, IMED Biotech Unit , AstraZeneca , 310, Cambridge Science Park, Milton Road , Cambridge CB4 0FZ , United Kingdom.
  • Perkins D; Oncology, IMED Biotech Unit , AstraZeneca , 310, Cambridge Science Park, Milton Road , Cambridge CB4 0FZ , United Kingdom.
  • Powell S; Oncology, IMED Biotech Unit , AstraZeneca , 310, Cambridge Science Park, Milton Road , Cambridge CB4 0FZ , United Kingdom.
  • Quesada MJ; Cancer Research UK, Therapeutic Discovery Laboratories , Jonas Webb Building, Babraham Research Campus , Cambridge CB22 3AT , United Kingdom.
  • Raubo P; Oncology, IMED Biotech Unit , AstraZeneca , 310, Cambridge Science Park, Milton Road , Cambridge CB4 0FZ , United Kingdom.
  • Sabin V; Cancer Research UK, Therapeutic Discovery Laboratories , Jonas Webb Building, Babraham Research Campus , Cambridge CB22 3AT , United Kingdom.
  • Smith J; Cancer Research UK, Therapeutic Discovery Laboratories , Jonas Webb Building, Babraham Research Campus , Cambridge CB22 3AT , United Kingdom.
  • Smith PD; Oncology, IMED Biotech Unit , AstraZeneca , 310, Cambridge Science Park, Milton Road , Cambridge CB4 0FZ , United Kingdom.
  • Stark A; Oncology, IMED Biotech Unit , AstraZeneca , 310, Cambridge Science Park, Milton Road , Cambridge CB4 0FZ , United Kingdom.
  • Ting A; Oncology, IMED Biotech Unit , AstraZeneca , 310, Cambridge Science Park, Milton Road , Cambridge CB4 0FZ , United Kingdom.
  • Wang P; Pharmaron Beijing Co., Ltd. , 6 Taihe Road, BDA , Beijing 100176 , P. R. China.
  • Wilson Z; Oncology, IMED Biotech Unit , AstraZeneca , 310, Cambridge Science Park, Milton Road , Cambridge CB4 0FZ , United Kingdom.
  • Winter-Holt JJ; Oncology, IMED Biotech Unit , AstraZeneca , 310, Cambridge Science Park, Milton Road , Cambridge CB4 0FZ , United Kingdom.
  • Wood JM; Oncology, IMED Biotech Unit , AstraZeneca , 310, Cambridge Science Park, Milton Road , Cambridge CB4 0FZ , United Kingdom.
  • Wrigley GL; Oncology, IMED Biotech Unit , AstraZeneca , 310, Cambridge Science Park, Milton Road , Cambridge CB4 0FZ , United Kingdom.
  • Yu G; Pharmaron Beijing Co., Ltd. , 6 Taihe Road, BDA , Beijing 100176 , P. R. China.
  • Zhang P; Pharmaron Beijing Co., Ltd. , 6 Taihe Road, BDA , Beijing 100176 , P. R. China.
J Med Chem ; 62(14): 6540-6560, 2019 07 25.
Article in En | MEDLINE | ID: mdl-31199640

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyridazines / Thiadiazoles / Glutaminase / Neoplasms / Antineoplastic Agents Limits: Animals / Humans / Male Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2019 Document type: Article Affiliation country: United kingdom Country of publication: United States

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyridazines / Thiadiazoles / Glutaminase / Neoplasms / Antineoplastic Agents Limits: Animals / Humans / Male Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2019 Document type: Article Affiliation country: United kingdom Country of publication: United States