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Discovery of 5-(1H-indol-5-yl)-1,3,4-thiadiazol-2-amines as potent PIM inhibitors
- Source :
- Bioorganic & Medicinal Chemistry Letters. 25:775-780
- Publication Year :
- 2015
- Publisher :
- Elsevier BV, 2015.
-
Abstract
- PIM kinases are a family of Ser/Thr kinases that are implicated in tumorigenesis. The discovery of a new class of PIM inhibitors, 5-(1H-indol-5-yl)-1,3,4-thiadiazol-2-amines, is discussed with optimized compounds showing excellent potency against all three PIM isoforms.
- Subjects :
- Models, Molecular
Gene isoform
Clinical Biochemistry
Pharmaceutical Science
medicine.disease_cause
Biochemistry
Structure-Activity Relationship
Proto-Oncogene Proteins c-pim-1
Cell Line, Tumor
hemic and lymphatic diseases
Drug Discovery
medicine
Humans
Potency
Structure–activity relationship
Amines
Protein Kinase Inhibitors
Molecular Biology
Drug discovery
Chemistry
Kinase
Organic Chemistry
Pim kinases
Molecular Medicine
Carcinogenesis
Carbolines
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 25
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....4102f5f33a7997eb18aa2e1429e22aa2