posted on 2015-12-17, 04:21authored byHui Wang, Chunying Yang, Joanne R. Doherty, William
R. Roush, John L. Cleveland, Thomas D. Bannister
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 14C-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.