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Potent blockers of the monocarboxylate transporter MCT1: Novel immunomodulatory compounds
- Source :
- Bioorganic & Medicinal Chemistry Letters. 16:2260-2265
- Publication Year :
- 2006
- Publisher :
- Elsevier BV, 2006.
-
Abstract
- A novel series of potent blockers of the monocarboxylate transporter, MCT1, is disclosed. From very potent but lipophilic lead compounds, systematic changes to all parts of the molecule, targeting reduction in log D, afforded compounds with significantly improved overall properties. These compounds show potent immunomodulatory activity.
- Subjects :
- Monocarboxylic Acid Transporters
T-Lymphocytes
Clinical Biochemistry
Graft vs Host Disease
Pharmaceutical Science
Biochemistry
Chemical synthesis
Cytochrome P-450 Enzyme System
Drug Discovery
Animals
Cytochrome P-450 CYP3A
Humans
Immunologic Factors
Molecular Biology
Herpesviridae
Cytochrome P-450 CYP2C9
Monocarboxylate transporter
chemistry.chemical_classification
Symporters
biology
Chemistry
Organic Chemistry
Antagonist
Cytochrome P450
Biological activity
Transporter
In vitro
Enzyme
biology.protein
Molecular Medicine
Aryl Hydrocarbon Hydroxylases
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 16
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....9008095be3d29fc103a2c186b3f3bb6d
- Full Text :
- https://doi.org/10.1016/j.bmcl.2006.01.024