Potent blockers of the monocarboxylate transporter MCT1: Novel immunomodulatory compounds

The synthesis and properties of a novel series of potent blockers of the monocarboxylate transporter, MCT1, are described. These compounds, exemplified by 30, show potent immunomodulatory activity. A novel series of potent blockers of the monocarboxylate transporter, MCT1, is disclosed. From very po...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-04, Vol.16 (8), p.2260-2265
Hauptverfasser:	Guile, S.D., Bantick, J.R., Cheshire, D.R., Cooper, M.E., Davis, A.M., Donald, D.K., Evans, R., Eyssade, C., Ferguson, D.D., Hill, S., Hutchinson, R., Ingall, A.H., Kingston, L.P., Martin, I., Martin, B.P., Mohammed, R.T., Murray, C., Perry, M.W.D., Reynolds, R.H., Thorne, P.V., Wilkinson, D.J., Withnall, J.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Aryl Hydrocarbon Hydroxylases - immunology Aryl Hydrocarbon Hydroxylases - metabolism Biological and medical sciences Cytochrome P-450 CYP2C9 Cytochrome P-450 CYP3A Cytochrome P-450 Enzyme System - immunology Cytochrome P-450 Enzyme System - metabolism Graft vs Host Disease - immunology Herpesviridae - drug effects Herpesviridae - immunology Herpesviridae - metabolism Humans Immunologic Factors - chemistry Immunologic Factors - pharmacology Immunomodulators Immunomodulatory Medical sciences Monocarboxylate Monocarboxylic Acid Transporters - antagonists & inhibitors Monocarboxylic Acid Transporters - immunology Monocarboxylic Acid Transporters - metabolism Pharmacology. Drug treatments Symporters - antagonists & inhibitors Symporters - immunology Symporters - metabolism T-Lymphocytes - drug effects T-Lymphocytes - immunology T-Lymphocytes - metabolism Transporter
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Beschreibung
Zusammenfassung:	The synthesis and properties of a novel series of potent blockers of the monocarboxylate transporter, MCT1, are described. These compounds, exemplified by 30, show potent immunomodulatory activity. 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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2006.01.024