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Imidazo[1,5-a]pyrazines: orally efficacious inhibitors of mTORC1 and mTORC2
- Source :
- Bioorganicmedicinal chemistry letters. 21(7)
- Publication Year :
- 2011
-
Abstract
- The discovery and optimization of a series of imidazo[1,5-a]pyrazine inhibitors of mTOR is described. HTS hits were optimized for potency, selectivity and metabolic stability to provide the orally bioavailable proof of concept compound 4c that demonstrated target inhibition in vivo and concomitant inhibition of tumor growth in an MDA-MB-231 xenograft model.
- Subjects :
- Models, Molecular
Pyrazine
Clinical Biochemistry
Pharmaceutical Science
Administration, Oral
Pharmacology
Mechanistic Target of Rapamycin Complex 1
Biochemistry
mTORC2
Chemical synthesis
chemistry.chemical_compound
In vivo
Oral administration
Cell Line, Tumor
Drug Discovery
Potency
Humans
Molecular Biology
PI3K/AKT/mTOR pathway
chemistry.chemical_classification
TOR Serine-Threonine Kinases
Organic Chemistry
Imidazoles
Proteins
Xenograft Model Antitumor Assays
Enzyme
chemistry
Multiprotein Complexes
Pyrazines
Molecular Medicine
Transcription Factors
Subjects
Details
- ISSN :
- 14643405
- Volume :
- 21
- Issue :
- 7
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....ba3d9f82c18f30d1e909a368b2bbd844