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Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4- d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N2-(2-Ethoxy-4-(4-methyl-4 H-1,2,4-triazol-3-yl)phenyl)-6-methyl- N8-neopentylpyrido[3,4- d]pyrimidine-2,8-diamine (BOS172722).
Woodward, Hannah L; Innocenti, Paolo; Cheung, Kwai-Ming J; Hayes, Angela; Roberts, Jennie; Henley, Alan T; Faisal, Amir; Mak, Grace Wing-Yan; Box, Gary; Westwood, Isaac M; Cronin, Nora; Carter, Michael; Valenti, Melanie; De Haven Brandon, Alexis; O'Fee, Lisa; Saville, Harry; Schmitt, Jessica; Burke, Rosemary; Broccatelli, Fabio; van Montfort, Rob L M; Raynaud, Florence I; Eccles, Suzanne A; Linardopoulos, Spiros; Blagg, Julian; Hoelder, Swen.
Afiliação
  • Woodward HL; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom.
  • Innocenti P; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom.
  • Cheung KJ; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom.
  • Hayes A; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom.
  • Roberts J; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom.
  • Henley AT; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom.
  • Faisal A; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom.
  • Mak GW; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom.
  • Box G; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom.
  • Westwood IM; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom.
  • Cronin N; Division of Structural Biology , The Institute of Cancer Research , London SW3 6JB , United Kingdom.
  • Carter M; Division of Structural Biology , The Institute of Cancer Research , London SW3 6JB , United Kingdom.
  • Valenti M; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom.
  • De Haven Brandon A; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom.
  • O'Fee L; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom.
  • Saville H; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom.
  • Schmitt J; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom.
  • Burke R; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom.
  • Broccatelli F; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom.
  • van Montfort RLM; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom.
  • Raynaud FI; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom.
  • Eccles SA; Division of Structural Biology , The Institute of Cancer Research , London SW3 6JB , United Kingdom.
  • Linardopoulos S; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom.
  • Blagg J; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom.
  • Hoelder S; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom.
J Med Chem ; 61(18): 8226-8240, 2018 09 27.
Article em En | MEDLINE | ID: mdl-30199249
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirimidinas / Triazóis / Proteínas Tirosina Quinases / Microssomos Hepáticos / Proteínas Serina-Treonina Quinases / Proteínas de Ciclo Celular / Inibidores de Proteínas Quinases / Descoberta de Drogas Tipo de estudo: Prognostic_studies Limite: Animals / Female / Humans / Male Idioma: En Revista: J Med Chem Ano de publicação: 2018 Tipo de documento: Article
Texto completo
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirimidinas / Triazóis / Proteínas Tirosina Quinases / Microssomos Hepáticos / Proteínas Serina-Treonina Quinases / Proteínas de Ciclo Celular / Inibidores de Proteínas Quinases / Descoberta de Drogas Tipo de estudo: Prognostic_studies Limite: Animals / Female / Humans / Male Idioma: En Revista: J Med Chem Ano de publicação: 2018 Tipo de documento: Article