作者: Konstantina Vougogiannopoulou , Alexios-Leandros Skaltsounis
关键词: Cyclin-dependent kinase 、 Biological activity 、 Biochemistry 、 Kinase 、 Molecular targets 、 Indirubin 、 Protein kinase A 、 Biology
摘要: Indirubins represent a small category of compounds with significant pharmacological activity focusing on the inhibition protein kinases. A series derivatives has been developed during last 15 years aiming investigation and amelioration indirubin scaffold in terms activity, selectivity, drug-likeness. The current article focuses naturally brominated indirubins present famous historic dye Tyrian purple, attempting to gather all available literature regarding biosynthesis, isolation, synthesis related analogues. Halogenated are by far one most important subcategories indirubins, its main representatives 6-bromoindirubin (6BI) 6-bromoindirubin-3′-oxime (6BIO) possessing an increased selectivity against GSK-3. This review attempts summarize concisely structure/activity relationships among closely halogenated analogues kinase while it also various biological applications arising from interactions molecular targets. Those include effects stem cells, cardiac, renal, pancreatic leukemia solid tumors, neurodegeneration.