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Impact of Minor Structural Modifications on Properties of a Series of mTOR Inhibitors.
Ouvry, Gilles; Clary, Laurence; Tomas, Loïc; Aurelly, Michèle; Bonnary, Laetitia; Borde, Emilie; Bouix-Peter, Claire; Chantalat, Laurent; Defoin-Platel, Claire; Deret, Sophie; Forissier, Mathieu; Harris, Craig S; Isabet, Tatiana; Lamy, Laurent; Luzy, Anne-Pascale; Pascau, Jonathan; Soulet, Catherine; Taddei, Alessandro; Taquet, Nathalie; Thoreau, Etienne; Varvier, Emeric; Vial, Emmanuel; Hennequin, Laurent F.
Afiliación
  • Ouvry G; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Clary L; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Tomas L; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Aurelly M; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Bonnary L; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Borde E; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Bouix-Peter C; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Chantalat L; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Defoin-Platel C; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Deret S; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Forissier M; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Harris CS; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Isabet T; Synchrotron Soleil, L'Orme des Merisiers, Saint-Aubin - BP 48, 91192 Gif-sur-Yvette Cedex, France.
  • Lamy L; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Luzy AP; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Pascau J; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Soulet C; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Taddei A; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Taquet N; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Thoreau E; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Varvier E; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Vial E; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Hennequin LF; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
ACS Med Chem Lett ; 10(11): 1561-1567, 2019 Nov 14.
Article en En | MEDLINE | ID: mdl-31749911
ABSTRACT
Minor structural modifications-sometimes single atom changes-can have a dramatic impact on the properties of compounds. This is illustrated here on structures related to known mTOR inhibitor Sapanisertib. Subtle changes in the hinge binder lead to strikingly different overall profiles with changes in physical properties, metabolism, and kinase selectivity.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: ACS Med Chem Lett Año: 2019 Tipo del documento: Article País de afiliación: Francia
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: ACS Med Chem Lett Año: 2019 Tipo del documento: Article País de afiliación: Francia