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Design, synthesis, and structure-activity-relationship of phenyl imidazoles as potent Smoothened antagonists
- Source :
- Bioorganicmedicinal chemistry letters. 22(21)
- Publication Year :
- 2012
-
Abstract
- Through scaffold morphing of a known Smoothened antagonist Antag691, a series of novel phenyl imidazole derivatives were developed. Structure-activity-relationship studies and lead optimization led to the discovery of potent, selective and orally bioavailable Smoothened antagonist 19 that is suitable for in vivo studies.
- Subjects :
- Stereochemistry
Clinical Biochemistry
Pharmaceutical Science
Administration, Oral
Antineoplastic Agents
Biochemistry
Receptors, G-Protein-Coupled
chemistry.chemical_compound
Inhibitory Concentration 50
Mice
Structure-Activity Relationship
In vivo
Drug Discovery
Structure–activity relationship
Inhibitory concentration 50
Imidazole
Animals
Humans
Molecular Biology
Chemistry
Organic Chemistry
Antagonist
Imidazoles
Combinatorial chemistry
Smoothened Receptor
Rats
Design synthesis
Area Under Curve
Drug Design
Molecular Medicine
Smoothened
Protein Binding
Subjects
Details
- ISSN :
- 14643405
- Volume :
- 22
- Issue :
- 21
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....6a4cae39d400bc2c17967bf41d17008e