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SAR towards indoline and 3-azaindoline classes of IDO1 inhibitors.
Yu, Wensheng; Deng, Yongqi; Hopkins, Brett; Huang, Xianhai; Sloman, David; Zhang, Hongjun; Li, Derun; McGowan, Meredeth A; White, Catherine; Pu, Qinglin; Liu, Kun; Fradera, Xavier; Lesburg, Charles A; Martinot, Theo; Doty, Amy; Ferguson, Heidi; Nickbarg, Elliott B; Cheng, Mangeng; Geda, Prasanthi; Song, Xuelei; Smotrov, Nadya; Abeywickrema, Pravien; Andrews, Christine; Chamberlin, Chad; Mabrouk, Omar; Curran, Patrick; Richards, Matthew; Saradjian, Peter; Miller, J Richard; Knemeyer, Ian; Otte, Karin; Vincent, Stella; Sciammetta, Nunzio; Bennett, David Jonathan; Han, Yongxin.
Afiliación
  • Yu W; Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA. Electronic address: wenshengyu@msn.com.
  • Deng Y; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Hopkins B; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Huang X; Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Sloman D; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Zhang H; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Li D; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • McGowan MA; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • White C; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Pu Q; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Liu K; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Fradera X; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Lesburg CA; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Martinot T; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Doty A; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Ferguson H; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Nickbarg EB; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Cheng M; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Geda P; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Song X; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Smotrov N; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Abeywickrema P; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Andrews C; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Chamberlin C; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Mabrouk O; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Curran P; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Richards M; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Saradjian P; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Miller JR; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Knemeyer I; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Otte K; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Vincent S; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Sciammetta N; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Bennett DJ; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Han Y; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Bioorg Med Chem Lett ; 47: 128214, 2021 09 01.
Article en En | MEDLINE | ID: mdl-34166782
ABSTRACT
A novel series of IDO1 inhibitors have been identified with good IDO1 Hela cell and human whole blood activity. These inhibitors contain an indoline or a 3-azaindoline scaffold. Their structure-activity-relationship studies have been explored. Compounds 37 and 41 stood out as leads due to their good potency in IDO1 Hela assay, good IDO1 unbound hWB IC50s, reasonable unbound clearance, and good MRT in rat and dog PK studies.
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Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Compuestos Aza / Indolamina-Pirrol 2,3,-Dioxigenasa / Indoles Límite: Animals / Humans / Male Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2021 Tipo del documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Compuestos Aza / Indolamina-Pirrol 2,3,-Dioxigenasa / Indoles Límite: Animals / Humans / Male Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2021 Tipo del documento: Article