Molecules, Vol. 25, Pages 2309: Development of Novel Analogs of the Monocarboxylate Transporter Ligand FACH and Biological Validation of One Potential Radiotracer for Positron Emission Tomography (PET) Imaging
Molecules, Vol. 25, Pages 2309: Development of Novel Analogs of the Monocarboxylate Transporter Ligand FACH and Biological Validation of One Potential Radiotracer for Positron Emission Tomography (PET) Imaging
Molecules doi: 10.3390/molecules25102309
Authors:
Masoud Sadeghzadeh
Barbara Wenzel
Daniel Gündel
Winnie Deuther-Conrad
Magali Toussaint
Rareş-Petru Moldovan
Steffen Fischer
Friedrich-Alexander Ludwig
Rodrigo Teodoro
Shirisha Jonnalagadda
Sravan K. Jonnalagadda
Gerrit Schüürmann
Venkatram R. Mereddy
Lester R. Drewes
Peter Brust
Monocarboxylate transporters 1-4 (MCT1-4) are involved in several metabolism-related diseases, especially cancer, providing the chance to be considered as relevant targets for diagnosis and therapy. [18F]FACH was recently developed and showed very promising preclinical results as a potential positron emission tomography (PET) radiotracer for imaging of MCTs. Given that [18F]FACH did not show high blood-brain barrier permeability, the current work is aimed to investigate whether more lipophilic analogs of FACH could improve brain uptake for imaging of gliomas, while retaining binding to MCTs. The 2-fluoropyridinyl-substituted analogs 1 and 2 were synthesized and their MCT1 inhibition was estimated by [14C]lactate uptake assay on rat brain endothelial-4 (RBE4) cells. While compounds 1 and 2 showed lower MCT1 inhibitory potencies than FACH (IC50 = 11 nM) by factors of 11 and 25, respectively, 1 (IC50 = 118 nM)...
Source: Molecules - Category: Chemistry Authors: Masoud Sadeghzadeh Barbara Wenzel Daniel G ündel Winnie Deuther-Conrad Magali Toussaint Rare ş-Petru Moldovan Steffen Fischer Friedrich-Alexander Ludwig Rodrigo Teodoro Shirisha Jonnalagadda Sravan K. Jonnalagadda Gerrit Sch üürmann Venkatram R. Mered Tags: Article Source Type: research
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