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Design and synthesis of pyrazolopyridine derivatives as sphingosine 1-phosphate receptor 2 ligands.
Luo, Zonghua; Yue, Xuyi; Yang, Hao; Liu, Hui; Klein, Robyn S; Tu, Zhude.
Afiliación
  • Luo Z; Department of Radiology, Washington University School of Medicine, St. Louis, MO 63110, USA.
  • Yue X; Department of Radiology, Washington University School of Medicine, St. Louis, MO 63110, USA.
  • Yang H; Department of Radiology, Washington University School of Medicine, St. Louis, MO 63110, USA.
  • Liu H; Department of Radiology, Washington University School of Medicine, St. Louis, MO 63110, USA.
  • Klein RS; Department of Medicine, Washington University School of Medicine, St. Louis, MO 63110, USA; Department of Neuroscience, Washington University School of Medicine, St. Louis, MO 63110, USA; Department of Pathology and Immunology, Washington University School of Medicine, St. Louis, MO 63110, USA.
  • Tu Z; Department of Radiology, Washington University School of Medicine, St. Louis, MO 63110, USA. Electronic address: tuz@mir.wustl.edu.
Bioorg Med Chem Lett ; 28(3): 488-496, 2018 02 01.
Article en En | MEDLINE | ID: mdl-29249563
Eleven new sphingosine 1-phosphate receptor 2 (S1PR2) ligands were synthesized by modifying lead compound N-(2,6-dichloropyridin-4-yl)-2-(4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)hydrazine-1-carboxamide (JTE-013) and their binding affinities toward S1PRs were determined in vitro using [32P]S1P and cell membranes expressing recombinant human S1PRs. Among these ligands, 35a (IC50 = 29.1 ±â€¯2.6 nM) and 35b (IC50 = 56.5 ±â€¯4.0 nM) exhibit binding potency toward S1PR2 comparable to JTE-013 (IC50 = 58.4 ±â€¯7.4 nM) with good selectivity for S1PR2 over the other S1PRs (IC50 > 1000 nM). Further optimization of these analogues may identify additional and more potent and selective compounds targeting S1PR2.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirazoles / Piridinas / Diseño de Fármacos / Receptores de Lisoesfingolípidos Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2018 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirazoles / Piridinas / Diseño de Fármacos / Receptores de Lisoesfingolípidos Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2018 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido