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Bioorg Med Chem Lett. 2006 Apr 15;16(8):2260-5. Epub 2006 Feb 7.

Potent blockers of the monocarboxylate transporter MCT1: novel immunomodulatory compounds.

Author information

1
Department of Medicinal Chemistry, AstraZeneca R&D Charnwood, Bakewell Road, Loughborough, LE11 5RH, UK. simon.guile@astrazeneca.com

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.

PMID:
16455256
DOI:
10.1016/j.bmcl.2006.01.024
[Indexed for MEDLINE]

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