Back to Search
Start Over
SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors
- Source :
- Bioorganicmedicinal chemistry letters. 20(5)
- Publication Year :
- 2009
-
Abstract
- The SAR of PXR transactivation by 3-(benzimidazol-2-yl)-pyridine-2-one based ATP competitive inhibitors of Insulin-like Growth Factor 1 Receptor kinase (IGF-1R) is discussed. Compounds without PXR transactivation, with in vivo antitumor activity, reduced protein binding and improved oral exposure are presented.
- Subjects :
- Transcriptional Activation
Benzimidazole
Receptors, Steroid
medicine.medical_treatment
Clinical Biochemistry
Pharmaceutical Science
Administration, Oral
Mice, Nude
Antineoplastic Agents
Plasma protein binding
digestive system
Biochemistry
Receptor, IGF Type 1
chemistry.chemical_compound
Transactivation
Mice
Structure-Activity Relationship
In vivo
Cell Line, Tumor
Drug Discovery
medicine
Animals
Cytochrome P-450 CYP3A
Humans
Receptor
Molecular Biology
Protein Kinase Inhibitors
Pregnane X receptor
Kinase
Growth factor
Organic Chemistry
Pregnane X Receptor
Xenograft Model Antitumor Assays
digestive system diseases
chemistry
Cancer research
Molecular Medicine
Benzimidazoles
Protein Binding
Subjects
Details
- ISSN :
- 14643405
- Volume :
- 20
- Issue :
- 5
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....13894aac7ddfa8d58651e185aff97076