Synthesis, Preclinical Evaluation, and First-in-Human PET Study of Quinoline-Containing PSMA Tracers with Decreased Renal Excretion

The prostate-specific membrane antigen (PSMA) is considered to be an excellent theranostic target of prostate cancer (PCa). In this study, three 18F-labeled PSMA tracers with a more lipophilic quinoline functional spacer were designed, synthesized, and evaluated based on the Glu-Ureido-Lys binding m...

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Veröffentlicht in:	Journal of medicinal chemistry 2021-04, Vol.64 (7), p.4179-4195
Hauptverfasser:	Zhang, Xiaojun, Wu, Yitian, Zeng, Qi, Xie, Tianxin, Yao, Shulin, Zhang, Jinming, Cui, Mengchao
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antigens, Surface - metabolism Cell Line, Tumor Contrast Media - chemical synthesis Contrast Media - chemistry Fluorine Radioisotopes - chemistry Glutamate Carboxypeptidase II - metabolism Humans Macaca fascicularis Male Mice Mice, Inbred ICR Positron-Emission Tomography Prostatic Neoplasms - diagnostic imaging Prostatic Neoplasms - metabolism Quinolines - chemical synthesis Quinolines - chemistry Quinolines - urine Radiopharmaceuticals - chemical synthesis Radiopharmaceuticals - chemistry Radiopharmaceuticals - urine Renal Elimination Urea - analogs & derivatives Urea - chemical synthesis Urea - urine
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