2. Academic Validation
  3. Synthesis and structure-activity relationships of pteridine dione and trione monocarboxylate transporter 1 inhibitors

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

  • J Med Chem. 2014 Sep 11;57(17):7317-24. doi: 10.1021/jm500640x.
Hui Wang 1,  Chunying Yang,  Joanne R Doherty,  William R Roush,  John L Cleveland,  Thomas D Bannister
Affiliations

Affiliation

  • 1 Department of Chemistry, The Scripps Research Institute , 130 Scripps Way, Jupiter, Florida 33458, United States.
PMID: 25068893 DOI: 10.1021/jm500640x
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.

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