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Synthesis and structure-activity relationships of pteridine dione and trione monocarboxylate transporter 1 inhibitors

Academic Article
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Overview

authors

  • Wang, H.
  • Yang, C.
  • Doherty, J. R.
  • Roush, William
  • Cleveland, John
  • Bannister, Thomas

publication date

  • September 2014

journal

  • Journal of Medicinal Chemistry  Journal

abstract

  • Novel substituted pteridine-derived inhibitors of monocarboxylate transporter 1 (MCT1), an emerging target for cancer therapy, are reported. The activity of these compounds as inhibitors of lactate transport was confirmed using a (14)C-lactate transport assay, and their potency against MCT1-expressing human tumor cells was established using MTT assays. The four most potent compounds showed substantial anticancer activity (EC50 37-150 nM) vs MCT1-expressing human Raji lymphoma cells.

subject areas

  • Animals
  • Antineoplastic Agents
  • Biological Transport
  • Cell Line, Tumor
  • Cell Survival
  • Dose-Response Relationship, Drug
  • Humans
  • Lactic Acid
  • MCF-7 Cells
  • Mice
  • Models, Chemical
  • Molecular Structure
  • Monocarboxylic Acid Transporters
  • Pteridines
  • Structure-Activity Relationship
  • Symporters
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Identity

PubMed Central ID

  • PMC4161152

International Standard Serial Number (ISSN)

  • 0022-2623

Digital Object Identifier (DOI)

  • 10.1021/jm500640x

PubMed ID

  • 25068893
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Additional Document Info

start page

  • 7317

end page

  • 7324

volume

  • 57

issue

  • 17

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