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

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.

SUBMITTER: Wang H 

PROVIDER: S-EPMC4161152 | biostudies-literature | 2014 Sep

REPOSITORIES: biostudies-literature