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Hit-to-lead optimization of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of KDR kinase inhibitors.
Dinges, Jürgen; Akritopoulou-Zanze, Irini; Arnold, Lee D; Barlozzari, Teresa; Bousquet, Peter F; Cunha, George A; Ericsson, Anna M; Iwasaki, Nobuhiko; Michaelides, Michael R; Ogawa, Nobuo; Phelan, Kathleen M; Rafferty, Paul; Sowin, Thomas J; Stewart, Kent D; Tokuyama, Ryukou; Xia, Zhiren; Zhang, Henry Q.
Afiliación
  • Dinges J; Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064-6101, USA. dinges@abbott.com
Bioorg Med Chem Lett ; 16(16): 4371-5, 2006 Aug 15.
Article en En | MEDLINE | ID: mdl-16750628
A series of 1,4-dihydroindeno[1,2-c]pyrazoles was prepared and evaluated for their enzymatic inhibition of KDR kinase. Computer modeling studies revealed the importance of attaching a basic side chain in predicting the binding mode of those compounds. Further investigation of structure-activity relationships led to 19, a lead compound with an acceptable selectivity profile, activity in whole cells, and good oral efficacy in an estradiol-induced murine uterine edema model of VEGF activity.
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirazoles / Indenos Tipo de estudio: Prognostic_studies Límite: Animals Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2006 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido
Buscar en Google
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PubMed Links

Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirazoles / Indenos Tipo de estudio: Prognostic_studies Límite: Animals Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2006 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido