التفاصيل البيبلوغرافية
العنوان:
Design and synthesis of dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole oximes as potent dual inhibitors of TIE-2 and VEGF-R2 receptor tyrosine kinases
المؤلفون:
Edward R. Bacon , Robert L. Hudkins , Thelma S. Angeles , Jennifer Grobelny , Mark S. Albom , Reddeppareddy Dandu , Bruce Ruggeri , Sheila J. Miknyoczki , Lisa D. Aimone , Shi Yang , Candy Robinson , Hong Chang , Allison L. Zulli , Ted L. Underiner
المصدر:
Bioorganic & Medicinal Chemistry Letters . 18:1916-1921
بيانات النشر:
Elsevier BV, 2008.
سنة النشر:
2008
مصطلحات موضوعية:
Umbilical Veins , Hemangiosarcoma , Clinical Biochemistry , Melanoma, Experimental , Administration, Oral , Pharmaceutical Science , Angiogenesis Inhibitors , Biochemistry , Chemical synthesis , Receptor tyrosine kinase , Structure-Activity Relationship , chemistry.chemical_compound , Oximes , Drug Discovery , Animals , Humans , Structure–activity relationship , Receptor , Protein Kinase Inhibitors , Molecular Biology , Cells, Cultured , Cell Proliferation , chemistry.chemical_classification , Molecular Structure , Neovascularization, Pathologic , biology , Organic Chemistry , Oxime , Receptor, TIE-2 , Vascular Endothelial Growth Factor Receptor-2 , Rats , Enzyme , chemistry , Enzyme inhibitor , Drug Design , biology.protein , Molecular Medicine , Endothelium, Vascular , Signal transduction
الوصف:
Fused dihydroindazolopyrrolocarbazole oximes have been identified as low nanomolar, potent dual TIE-2 and VEGF-R2 receptor tyrosine kinase inhibitors with excellent cellular potency. Development of the structure-activity relationships (SAR) led to identification of compounds 35 and 40 as potent, selective dual TIE-2/VEGF-R2 inhibitors with favorable pharmacokinetic properties. Compound 35 was orally active in tumor models with no observed toxicity.
تدمد:
0960-894X
URL الوصول:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ff81dd5bd91b90c842800ca27629d74b https://doi.org/10.1016/j.bmcl.2008.02.001
حقوق:
CLOSED
رقم الأكسشن:
edsair.doi.dedup.....ff81dd5bd91b90c842800ca27629d74b
قاعدة البيانات:
OpenAIRE
