2. Academic Validation
  3. Potent blockers of the monocarboxylate transporter MCT1: novel immunomodulatory compounds

Potent blockers of the monocarboxylate transporter MCT1: novel immunomodulatory compounds

  • Bioorg Med Chem Lett. 2006 Apr 15;16(8):2260-5. doi: 10.1016/j.bmcl.2006.01.024.
S D Guile 1,  J R Bantick,  D R Cheshire,  M E Cooper,  A M Davis,  D K Donald,  R Evans,  C Eyssade,  D D Ferguson,  S Hill,  R Hutchinson,  A H Ingall,  L P Kingston,  I Martin,  B P Martin,  R T Mohammed,  C Murray,  M W D Perry,  R H Reynolds,  P V Thorne,  D J Wilkinson,  J Withnall
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, AstraZeneca R&D Charnwood, Bakewell Road, Loughborough, LE11 5RH, UK. simon.guile@astrazeneca.com
PMID: 16455256 DOI: 10.1016/j.bmcl.2006.01.024
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.

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