Journal of medicinal chemistry, 2014-09, Vol.57 (17), p.7317-7324
2014
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Details
- Autor(en) / Beteiligte
- Titel
- Synthesis and Structure–Activity Relationships of Pteridine Dione and Trione Monocarboxylate Transporter 1 Inhibitors
- Ist Teil von
- Journal of medicinal chemistry, 2014-09, Vol.57 (17), p.7317-7324
- Ort / Verlag
- United States: American Chemical Society
- Erscheinungsjahr
- 2014
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- 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.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0022-2623eISSN: 1520-4804DOI: 10.1021/jm500640xTitel-ID: cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_4161152
- Format
- –
- Schlagworte
- Animals, Antineoplastic Agents - chemical synthesis, Antineoplastic Agents - chemistry, Antineoplastic Agents - pharmacology, Biological Transport - drug effects, Cell Line, Tumor, Cell Survival - drug effects, Dose-Response Relationship, Drug, Humans, Lactic Acid - metabolism, MCF-7 Cells, Mice, Models, Chemical, Molecular Structure, Monocarboxylic Acid Transporters - antagonists & inhibitors, Monocarboxylic Acid Transporters - metabolism, Pteridines - chemical synthesis, Pteridines - chemistry, Pteridines - pharmacology, Structure-Activity Relationship, Symporters - antagonists & inhibitors, Symporters - metabolism