Indazolylpyrazolopyrimidine as Highly Potent B-Raf Inhibitors with in Vivo Activity
| العنوان: | Indazolylpyrazolopyrimidine as Highly Potent B-Raf Inhibitors with in Vivo Activity |
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| المؤلفون: | Karen Collins, Donald Wojciechowicz, Judy Lucas, Nancy Torres, Jeremy I. Levin, Yongbo Hu, Cilien Hanna, Dan M. Berger, Edward J. Salaski, Eileen Frommer, Minu Dutia, Wang Xiaolun, Dennis Powell |
| المصدر: | Journal of Medicinal Chemistry. 53:7874-7878 |
| بيانات النشر: | American Chemical Society (ACS), 2010. |
| سنة النشر: | 2010 |
| مصطلحات موضوعية: | Models, Molecular, Proto-Oncogene Proteins B-raf, Indazoles, Transplantation, Heterologous, Mutant, Antineoplastic Agents, Pharmacology, Mice, Structure-Activity Relationship, Pyrimidine analogue, chemistry.chemical_compound, Pharmacokinetics, In vivo, Cell Line, Tumor, Drug Discovery, Animals, Humans, Chemistry, Kinase, Bridged Bicyclo Compounds, Heterocyclic, humanities, Pyrimidines, Biochemistry, Mutation, Pyrazoles, Molecular Medicine, Drug Screening Assays, Antitumor, Selectivity, Lead compound, Neoplasm Transplantation |
| الوصف: | Novel indazolylpyrazolo[1,5-a]pyrimidine analogues have been prepared and found to be extremely potent type I B-Raf inhibitors. The lead compound shows good selectivity against a panel of 60 kinases, possesses a desirable pharmacokinetic profile, and demonstrates excellent in vivo antitumor efficacy in B-Raf mutant xenograft models. |
| تدمد: | 1520-4804 0022-2623 |
| الوصول الحر: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f5cfb7f80cde520202634116ccfc59adTest https://doi.org/10.1021/jm1007566Test |
| رقم الانضمام: | edsair.doi.dedup.....f5cfb7f80cde520202634116ccfc59ad |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 15204804 00222623 |
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