Development of radiofluorinated nicotinamide/picolinamide derivatives as diagnostic probes for the detection of melanoma

Yi Hsuan Lo, Ting Yu Chang, Chuan Lin Chen, Ming Hsien Lin, Hsin Ell Wang, Chi Wei Chang, Ren Shyan Liu, Chun Yi Wu*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

1 Scopus citations

Abstract

Regarding the increased incidence and high mortality rate of malignant melanoma, practical early-detection methods are essential to improve patients’ clinical outcomes. In this study, we successfully prepared novel picolinamide–benzamide (18 F-FPABZA) and nicotinamide–benzamide (18 F-FNABZA) conjugates and determined their biological characteristics. The radiochemical yields of18 F-FPABZA and18 F-FNABZA were 26 ± 5% and 1 ± 0.5%, respectively.18 F-FPABZA was more lipophilic (log P = 1.48) than18 F-FNABZA (log P = 0.68). The cellular uptake of18 F-FPABZA in melanotic B16F10 cells was relatively higher than that of18 F-FNABZA at 15 min post-incubation. However, both radiotracers did not retain in amelanotic A375 cells. The tumor-to-muscle ratios of18 F-FPABZA-injected B16F10 tumor-bearing mice increased from 7.6 ± 0.4 at 15 min post-injection (p.i.) to 27.5 ± 16.6 at 3 h p.i., while those administered with18 F-FNABZA did not show a similarly dramatic increase throughout the experimental period. The results obtained from biodistribution studies were consistent with those derived from microPET imaging. This study demonstrated that18 F-FPABZA is a promising melanin-targeting positron emission tomography (PET) probe for melanotic melanoma.

Original languageEnglish
Article number6432
JournalInternational Journal Of Molecular Sciences
Volume22
Issue number12
DOIs
StatePublished - 2 Jun 2021

Keywords

  • Melanin-targeting probe
  • Melanoma
  • Radioflu-orinated nicotinamide–benzamide derivative ( F-FNABZA)
  • Radiofluorinated picolinamide–benzamide derivative ( F-FPABZA)

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