Journal Article Bioorganic & Medicinal Chemistry Letters

Tateishi, Hiroyuki  ,  Tsuji, Atsushi  ,  Kato, Koichi  ,  Sudo, Hitomi  ,  Sugyo, Aya  ,  Hanakawa, Takashi  ,  Ming-Rong, Zhang  ,  Saga, Tsuneo  ,  Yasushi, Arano  ,  Higashi, Tatsuya

Description
Upregulated monocarboxylate transporters (MCTs) in tumors are considered diagnostic imaging targets.Herein, we synthesized the positron emission tomography probe candidates coumarin analogs 2 and 3,and showed 55 times higher affinity of 2 for MCTs than a representative MCT inhibitor. Whereas [11C]2 showed low tumor accumulation, probably due to adduct formation with plasma proteins, [11C]2showed high initial brain uptake, suggesting that the scaffold of 2 has properties that are preferable inimaging probes for the astrocyte–neuron lactate shuttle. Although further optimization of 2 is required,our findings can be used to inform the development of MCT-targeted imaging agents. 2017 The Author(s). Published by Elsevier Ltd. This is an open access article under the CC BY license

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