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Scaffold hopping towards potent and selective JAK3 inhibitors: discovery of novel C-5 substituted pyrrolopyrazines.
de Vicente, Javier; Lemoine, Remy; Bartlett, Mark; Hermann, Johannes C; Hekmat-Nejad, Mohammad; Henningsen, Robert; Jin, Sue; Kuglstatter, Andreas; Li, Hongju; Lovey, Allen J; Menke, John; Niu, Linghao; Patel, Vaishali; Petersen, Ann; Setti, Lina; Shao, Ada; Tivitmahaisoon, Parcharee; Vu, Minh Diem; Soth, Michael.
Afiliación
  • de Vicente J; Small Molecule Research, Pharma Research & Early Development, pRED, Hoffmann-La Roche Inc., 340 Kingsland Street, Nutley, NJ 07110, United States. Electronic address: javier.devicente@novartis.com.
  • Lemoine R; Roche Palo Alto, 3401 Hillview Ave, Palo Alto, CA 94304, United States.
  • Bartlett M; Roche Palo Alto, 3401 Hillview Ave, Palo Alto, CA 94304, United States.
  • Hermann JC; Small Molecule Research, Pharma Research & Early Development, pRED, Hoffmann-La Roche Inc., 340 Kingsland Street, Nutley, NJ 07110, United States.
  • Hekmat-Nejad M; Roche Palo Alto, 3401 Hillview Ave, Palo Alto, CA 94304, United States.
  • Henningsen R; Roche Palo Alto, 3401 Hillview Ave, Palo Alto, CA 94304, United States.
  • Jin S; Small Molecule Research, Pharma Research & Early Development, pRED, Hoffmann-La Roche Inc., 340 Kingsland Street, Nutley, NJ 07110, United States.
  • Kuglstatter A; Small Molecule Research, Pharma Research & Early Development, pRED, Hoffmann-La Roche Inc., 340 Kingsland Street, Nutley, NJ 07110, United States.
  • Li H; Small Molecule Research, Pharma Research & Early Development, pRED, Hoffmann-La Roche Inc., 340 Kingsland Street, Nutley, NJ 07110, United States.
  • Lovey AJ; Small Molecule Research, Pharma Research & Early Development, pRED, Hoffmann-La Roche Inc., 340 Kingsland Street, Nutley, NJ 07110, United States.
  • Menke J; Small Molecule Research, Pharma Research & Early Development, pRED, Hoffmann-La Roche Inc., 340 Kingsland Street, Nutley, NJ 07110, United States.
  • Niu L; Small Molecule Research, Pharma Research & Early Development, pRED, Hoffmann-La Roche Inc., 340 Kingsland Street, Nutley, NJ 07110, United States.
  • Patel V; Small Molecule Research, Pharma Research & Early Development, pRED, Hoffmann-La Roche Inc., 340 Kingsland Street, Nutley, NJ 07110, United States.
  • Petersen A; Small Molecule Research, Pharma Research & Early Development, pRED, Hoffmann-La Roche Inc., 340 Kingsland Street, Nutley, NJ 07110, United States.
  • Setti L; Roche Palo Alto, 3401 Hillview Ave, Palo Alto, CA 94304, United States.
  • Shao A; Roche Palo Alto, 3401 Hillview Ave, Palo Alto, CA 94304, United States.
  • Tivitmahaisoon P; Small Molecule Research, Pharma Research & Early Development, pRED, Hoffmann-La Roche Inc., 340 Kingsland Street, Nutley, NJ 07110, United States.
  • Vu MD; Small Molecule Research, Pharma Research & Early Development, pRED, Hoffmann-La Roche Inc., 340 Kingsland Street, Nutley, NJ 07110, United States.
  • Soth M; Small Molecule Research, Pharma Research & Early Development, pRED, Hoffmann-La Roche Inc., 340 Kingsland Street, Nutley, NJ 07110, United States.
Bioorg Med Chem Lett ; 24(21): 4969-75, 2014 Nov 01.
Article en En | MEDLINE | ID: mdl-25262541
The discovery of a novel series of pyrrolopyrazines as JAK inhibitors with comparable enzyme and cellular activity to tofacitinib is described. The series was identified using a scaffold hopping approach aided by structure based drug design using principles of intramolecular hydrogen bonding for conformational restriction and targeting specific pockets for modulating kinase activity.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirazinas / Pirroles / Inhibidores de Proteínas Quinasas / Janus Quinasa 3 Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2014 Tipo del documento: Article Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirazinas / Pirroles / Inhibidores de Proteínas Quinasas / Janus Quinasa 3 Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2014 Tipo del documento: Article Pais de publicación: Reino Unido