Synthesis and Structure鈥揂ctivity Relationships of Pteridine Dione and Trione Monocarboxylate Transporter 1 Inhibitors

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• 作者：Hui Wang ; Chunying Yang ; Joanne R. Doherty ; William R. Roush ; John L. Cleveland ; Thomas D. Bannister
• 刊名：Journal of Medicinal Chemistry
• 出版年：2014
• 出版时间：September 11, 2014
• 年：2014
• 卷：57
• 期：17
• 页码：7317-7324
• 全文大小：380K
• ISSN：1520-4804

文摘

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鈥?50 nM) vs MCT1-expressing human Raji lymphoma cells.