Synthesis and evaluation of 11C-labeled coumarin analog as an imaging probe for detecting monocarboxylate transporters expression. Issue 21 (1st November 2017)

• Record Type: Journal Article
• Authors: Tateishi, Hiroyuki; Tsuji, Atsushi B.; Kato, Koichi; Sudo, Hitomi; Sugyo, Aya; Hanakawa, Takashi; Zhang, Ming-Rong; Saga, Tsuneo; Arano, Yasushi; Higashi, Tatsuya
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 21(2017)
• Page Start: 4893
• Page End: 4897
• Publication Date: 2017-11-01
• Subjects: Positron emission tomography -- Fluorescence -- Cancer -- Astrocyte–neuron lactate shuttle -- Radiosynthesis; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.09.033
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: Upregulated monocarboxylate transporters (MCTs) in tumors are considered diagnostic imaging targets. Herein, we synthesized the positron emission tomography probe candidates coumarin analogs2 and3, and showed 55 times higher affinity of2 for MCTs than a representative MCT inhibitor. Whereas[ 11 C]2 showed low tumor accumulation, probably due to adduct formation with plasma proteins, [ 11 C]2 showed high initial brain uptake, suggesting that the scaffold of2 has properties that are preferable in imaging probes for the astrocyte–neuron lactate shuttle. Although further optimization of2 is required, our findings can be used to inform the development of MCT-targeted imaging agents.